The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Carbamates in which the -CO- group has been replaced by a -CS- group.
A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
Exclusive legal rights or privileges applied to inventions, plants, etc.
Neutral or negatively charged ligands bonded to metal cations or neutral atoms. The number of ligand atoms to which the metal center is directly bonded is the metal cation's coordination number, and this number is always greater than the regular valence or oxidation number of the metal. A coordination complex can be negative, neutral, or positively charged.
Cyclic AMIDES formed from aminocarboxylic acids by the elimination of water. Lactims are the enol forms of lactams.
A class of compounds of the type R-M, where a C atom is joined directly to any other element except H, C, N, O, F, Cl, Br, I, or At. (Grant & Hackh's Chemical Dictionary, 5th ed)
A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.
Property, such as patents, trademarks, and copyright, that results from creative effort. The Patent and Copyright Clause (Art. 1, Sec. 8, cl. 8) of the United States Constitution provides for promoting the progress of science and useful arts by securing for limited times to authors and inventors, the exclusive right to their respective writings and discoveries. (From Black's Law Dictionary, 5th ed, p1014)
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.
Synthetic organic reactions that use reactions between unsaturated molecules to form cyclical products.
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Hydrocarbons with at least one triple bond in the linear portion, of the general formula Cn-H2n-2.
A plant genus of the family Cephalotaxaceae, order Pinales, class Pinopsida, division CONIFEROPHYTA. Members contain homoharringtonine.
Tetracyclic spiro-BENZAZEPINES isolated from the seeds of CEPHALOTAXUS. They are esters of the alkaloid cephalotaxine and may be effective as antineoplastic agents.
The aggregate enterprise of manufacturing and technically producing chemicals. (From Random House Unabridged Dictionary, 2d ed)
A genus of gram-negative, aerobic, nonsporeforming rods which usually contain granules of poly-beta-hydroxybutyrate. (From Bergey's Manual of Determinative Bacteriology, 9th ed)
Feeling or emotion of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.
Persistent and disabling ANXIETY.
Ubiquitous, inducible, nuclear transcriptional activator that binds to enhancer elements in many different cell types and is activated by pathogenic stimuli. The NF-kappa B complex is a heterodimer composed of two DNA-binding subunits: NF-kappa B1 and relA.
Naturally occurring or synthetic substances that inhibit or retard the oxidation of a substance to which it is added. They counteract the harmful and damaging effects of oxidation in animal tissues.
The N-acetyl derivative of CYSTEINE. It is used as a mucolytic agent to reduce the viscosity of mucous secretions. It has also been shown to have antiviral effects in patients with HIV due to inhibition of viral stimulation by reactive oxygen intermediates.

Different contributions of endothelin-A and endothelin-B receptors in the pathogenesis of deoxycorticosterone acetate-salt-induced hypertension in rats. (1/1906)

We investigated the involvement of actions mediated by endothelin-A (ETA) and endothelin-B (ETB) receptors in the pathogenesis of deoxycorticosterone acetate (DOCA)-salt-induced hypertension in rats. Two weeks after the start of DOCA-salt treatment, rats were given ABT-627 (10 [mg/kg]/d), a selective ETA receptor antagonist; A-192621 (30 [mg/kg]/d), a selective ETB receptor antagonist; or their vehicle for 2 weeks. Uninephrectomized rats without DOCA-salt treatment served as controls. Treatment with DOCA and salt for 2 weeks led to a mild but significant hypertension; in vehicle-treated DOCA-salt rats, systolic blood pressure increased markedly after 3 to 4 weeks. Daily administration of ABT-627 for 2 weeks almost abolished any further increases in blood pressure, whereas A-192621 did not affect the development of DOCA-salt-induced hypertension. When the degree of vascular hypertrophy of the aorta was histochemically evaluated at 4 weeks, there were significant increases in wall thickness, wall area, and wall-to-lumen ratio in vehicle-treated DOCA-salt rats compared with uninephrectomized control rats. The development of vascular hypertrophy was markedly suppressed by ABT-627. In contrast, treatment with A-192621 significantly exaggerated these vascular changes. In vehicle-treated DOCA-salt rats, renal blood flow and creatinine clearance decreased, and urinary excretion of protein, blood urea nitrogen, fractional excretion of sodium, and urinary N-acetyl-beta-glucosaminidase activity increased. Such damage was overcome by treatment with ABT-627 but not with A-192621; indeed, the latter agent led to worsening of the renal dysfunction. Histopathologic examination of the kidney in vehicle-treated DOCA-salt rats revealed tubular dilatation and atrophy as well as thickening of small arteries. Such damage was reduced in animals given ABT-627, whereas more severe histopathologic changes were observed in A-192621-treated animals. These results strongly support the view that ETA receptor-mediated action plays an important role in the pathogenesis of DOCA-salt-induced hypertension. On the other hand, it seems likely that the ETB receptor-mediated action protects against vascular and renal injuries in this model of hypertension. A selective ETA receptor antagonist is likely to be useful for treatment of subjects with mineralocorticoid-dependent hypertension, whereas ETB-selective antagonism alone is detrimental to such cases.  (+info)

S-16924 [(R)-2-[1-[2-(2,3-dihydro-benzo[1,4]dioxin-5-yloxy)-ethyl]- pyrrolidin-3yl]-1-(4-fluorophenyl)-ethanone], a novel, potential antipsychotic with marked serotonin1A agonist properties: III. Anxiolytic actions in comparison with clozapine and haloperidol. (2/1906)

S-16924 is a potential antipsychotic that displays agonist and antagonist properties at serotonin (5-HT)1A and 5-HT2A/2C receptors, respectively. In a pigeon conflict procedure, the benzodiazepine clorazepate (CLZ) increased punished responses, an action mimicked by S-16924, whereas the atypical antipsychotic clozapine and the neuroleptic haloperidol were inactive. Similarly, in a Vogel conflict paradigm in rats, CLZ increased punished responses, an action shared by S-16924 but not by clozapine or haloperidol. This action of S-16924 was abolished by the 5-HT1A antagonist WAY-100,635. Ultrasonic vocalizations in rats were inhibited by CLZ, S-16924, clozapine, and haloperidol. However, although WAY-100,635 abolished the action of S-16924, it did not affect clozapine and haloperidol. In a rat elevated plus-maze, CLZ, but not S-16924, clozapine, and haloperidol, increased open-arm entries. Like CLZ, S-16924 increased social interaction in rats, whereas clozapine and haloperidol were inactive. WAY-100,635 abolished this action of S-16924. CLZ, S-16924, clozapine, and haloperidol decreased aggressive interactions in isolated mice, but this effect of S-16924 was not blocked by WAY-100, 635. All drugs inhibited motor behavior, but the separation to anxiolytic doses was more pronounced for S-16924 than for CLZ. Finally, in freely moving rats, CLZ and S-16924, but not clozapine and haloperidol, decreased dialysis levels of 5-HT in the nucleus accumbens: this action of S-16924 was blocked by WAY-100,165. In conclusion, in contrast to haloperidol and clozapine, S-16924 possessed a broad-based profile of anxiolytic activity at doses lower than those provoking motor disruption. Its principal mechanism of action was activation of 5-HT1A (auto)receptors.  (+info)

Increased lipophilicity and subsequent cell partitioning decrease passive transcellular diffusion of novel, highly lipophilic antioxidants. (3/1906)

Oxidative stress is considered a cause or propagator of acute and chronic disorders of the central nervous system. Novel 2, 4-diamino-pyrrolo[2,3-d]pyrimidines are potent inhibitors of iron-dependent lipid peroxidation, are cytoprotective in cell culture models of oxidative injury, and are neuroprotective in brain injury and ischemia models. The selection of lead candidates from this series required that they reach target cells deep within brain tissue in efficacious amounts after oral dosing. A homologous series of 26 highly lipophilic pyrrolopyrimidines was examined using cultured cell monolayers to understand the structure-permeability relationship and to use this information to predict brain penetration and residence time. Pyrrolopyrimidines were shown to be a more permeable structural class of membrane-interactive antioxidants where transepithelial permeability was inversely related to lipophilicity or to cell partitioning. Pyrrole substitutions influence cell partitioning where bulky hydrophobic groups increased partitioning and decreased permeability and smaller hydrophobic groups and more hydrophilic groups, especially those capable of weak hydrogen bonding, decreased partitioning, and increased permeability. Transmonolayer diffusion for these membrane-interactive antioxidants was limited mostly by desorption from the receiver-side membrane into the buffer. Thus, in this case, these in vitro cell monolayer models do not adequately mimic the in vivo situation by underestimating in vivo bioavailability of highly lipophilic compounds unless acceptors, such as serum proteins, are added to the receiving buffer.  (+info)

Novel, highly lipophilic antioxidants readily diffuse across the blood-brain barrier and access intracellular sites. (4/1906)

In an accompanying article, an in vitro assay for permeability predicts that membrane-protective, antioxidant 2,4-diamino-pyrrolo[2, 3-d]pyrimidines should have improved blood-brain barrier (BBB) permeation over previously described lipophilic antioxidants. Using a first-pass extraction method and brain/plasma quantification, we show here that two of the pyrrolopyrimidines, one of which is markedly less permeable, readily partition into rat brain. The efficiency of extraction was dependent on serum protein binding, and in situ efflux confirms the in vitro data showing that PNU-87663 is retained in brain longer than PNU-89843. By exploiting inherent fluorescence properties of PNU-87663, its distribution within brain and within cells in culture was demonstrated using confocal scanning laser microscopy. PNU-87663 rapidly partitioned into the cell membrane and equilibrates with cytoplasmic compartments via passive diffusion. Although partitioning of PNU-87663 favors intracytoplasmic lipid storage droplets, the compound was readily exchangeable as shown by efflux of compound from cells to buffer when protein was present. The results demonstrated that pyrrolopyrimidines were well suited for quickly accessing target cells within the central nervous system as well as in other target tissues.  (+info)

Pyrrolidine dithiocarbamate up-regulates the expression of the genes encoding the catalytic and regulatory subunits of gamma-glutamylcysteine synthetase and increases intracellular glutathione levels. (5/1906)

Time- and dose-dependent increases in the steady-state mRNA levels of the genes encoding the catalytic and regulatory subunits of the enzyme gamma-glutamylcysteine synthetase (GCS) were observed in HepG2 human hepatocarcinoma cells after exposure to pyrrolidine dithiocarbamate (PDTC). PDTC was demonstrated to manifest both antioxidant and pro-oxidant properties in HepG2 cells, as assessed by the decreased fluorescence of the redox-sensitive dye Dihydrorhodamine 123 and by the oxidation of glutathione respectively. Attempts to characterize the signalling pathway from PDTC exposure to increases in the expression of the GCS catalytic and regulatory subunit genes demonstrated that induction by PDTC could be partially blocked by treatment with the thiol agent N-acetylcysteine and by the copper chelator bathocuproine disulphonic acid. These findings suggested that the up-regulation of the two genes resulted from a PDTC-induced pro-oxidant signal, which was partially copper-dependent. In summary, these studies demonstrate that PDTC exposure elicits a cellular response in HepG2 cells, characterized by the induction of the genes encoding the two subunits of the enzyme GCS and increased de novo synthesis of the cellular protectant GSH.  (+info)

Endothelin stimulates glucose uptake and GLUT4 translocation via activation of endothelin ETA receptor in 3T3-L1 adipocytes. (6/1906)

Endothelin-1 (ET-1) is a 21-amino acid peptide that binds to G-protein-coupled receptors to evoke biological responses. This report studies the effect of ET-1 on regulating glucose transport in 3T3-L1 adipocytes. ET-1, but not angiotensin II, stimulated glucose uptake in a dose-dependent manner with an EC50 value of 0.29 nM and a 2.47-fold stimulation at 100 nM. ET-1 stimulated glucose uptake in differentiated 3T3-L1 cells but had no effect in undifferentiated cells, although ET-1 stimulated phosphatidylinositol hydrolysis to a similar degree in both. The 3T3-L1 cells expressed approximately 560,000 sites/cell of ETA receptor, which was not altered during differentiation. Western blot analysis and immunofluorescence staining show that ET-1 stimulated the translocation of insulin-responsive aminopeptidase and GLUT4 to the plasma membrane. The effect of ET-1 on glucose uptake was blocked by A-216546, an antagonist selective for the ETA receptor. ET-1 treatment did not induce phosphorylation of insulin receptor beta-subunit, insulin receptor substrate-1, or Akt but stimulated the tyrosyl phosphorylation of a 75-kDa protein. Genistein (100 microM), an inhibitor of tyrosine kinases, inhibited ET-1-stimulated glucose uptake. Our results show that ET-1 stimulates GLUT4 translocation and glucose uptake in 3T3-L1 adipocytes via activation of ETA receptor.  (+info)

Comparison of two aquaretic drugs (niravoline and OPC-31260) in cirrhotic rats with ascites and water retention. (7/1906)

kappa-Opioid receptor agonists (niravoline) or nonpeptide antidiuretic hormone (ADH) V2 receptor antagonists (OPC-31260) possess aquaretic activity in cirrhosis; however, there is no information concerning the effects induced by the chronic administration of these drugs under this condition. To compare the renal and hormonal effects induced by the long-term oral administration of niravoline, OPC-31260, or vehicle, urine volume, urinary osmolality, sodium excretion, and urinary excretion of aldosterone (ALD) and ADH were measured in basal conditions and for 10 days after the daily oral administration of niravoline, OPC-31260, or vehicle to cirrhotic rats with ascites and water retention. Creatinine clearance, serum osmolality, ADH mRNA expression, and systemic hemodynamics were also measured at the end of the study. Niravoline increased water excretion, peripheral resistance, serum osmolality, and sodium excretion and reduced creatinine clearance, ALD and ADH excretion, and mRNA expression of ADH. OPC-31260 also increased water metabolism and sodium excretion and reduced urinary ALD, although the aquaretic effect was only evident during the first 2 days, and no effects on serum osmolality, renal filtration, and systemic hemodynamics were observed. Therefore, both agents have aquaretic efficacy, but the beneficial therapeutic effects of the long-term oral administration of niravoline are more consistent than those of OPC-31260 in cirrhotic rats with ascites and water retention.  (+info)

S-16924, a novel, potential antipsychotic with marked serotonin1A agonist properties. IV. A drug discrimination comparison with clozapine. (8/1906)

The novel benzodioxopyrrolidine (S-16924) displays a clozapine-like profile of interaction with multiple monoaminergic receptors, in addition to potent agonist activity at serotonin (5-HT)1A receptors. S-16924 (2.5 mg/kg i.p.) and clozapine (5.0 mg/kg i.p.) generated robust discriminative stimuli (DS) and displayed full mutual generalization. The D4 antagonists L-745,870 and S-18126, the D1/D5 antagonist SCH-39166, and the D3 antagonist S-14297 showed at most partial generalization to S-16924 and clozapine. The D2/D3 antagonist raclopride fully generalized to S-16924, but only partially generalized to clozapine. The 5-HT2A antagonist MDL-100, 907 fully generalized to S-16924 and two further 5-HT2A antagonists, fananserin and SR-46349, showed partial generalization. However, MDL-100,907, fananserin, and SR-46349 showed less pronounced generalization to clozapine. Similarly, the 5-HT2C antagonists SB-200,646 and SB-206,553 more markedly generalized to S-16924 than to clozapine. The 5-HT1A receptor agonist (+/-)-8-dihydroxy-2-(di-n-propylamino) tetralin generalized fully to S-16924 but not to clozapine. Full generalization was obtained to both S-16924 and clozapine for the clozapine congeners, olanzapine and quetiapine. In distinction, the benzisoxazole, risperidone, and the phenylindole, sertindole, weakly generalized to S-16924 and clozapine. However, the benzisoxazole ziprasidone, which possesses 5-HT1A agonist properties, generalized fully to S-16924 but not to clozapine. Finally, the muscarinic antagonist scopolamine generalized fully to clozapine and partially to S-16924. In conclusion, S-16924 and clozapine display both communalities and differences in their "compound" DS; this likely reflects their respective complex patterns of interaction with multiple monoaminergic receptors. Although no specific receptor was identified as underlying the clozapine DS, 5-HT1A agonist as well as D2 and 5-HT2A/2C antagonist properties contribute to the S-16924 DS.  (+info)

Pyrrolidines are cyclic secondary amines with a five-membered ring, containing four carbon atoms and one nitrogen atom. The pyrrolidine ring is the central structure of the amino acid proline and its derivatives. Chiral pyrrolidines play an important role both as chiral building blocks for auxiliaries as well as key structures relevant to biologically active substances. Derivatives of the methylpyrrolidinyl fragment are common structural motifs present in several inhibitors and antagonists, including a series of HIV-1 reverse transcriptase inhibitors and histamine H3 receptor and dopamine D4 antagonists. Sigma-Aldrich has a large selection of pyrrolidines as heterocyclic building blocks for organic synthesis and medicinal chemistry, the majority of which are available as racemates or in either enantiomeric form.Learn More about PyrrolidinesPyrrolidines
Information for Pyrrolidine 123-75-1 including Pyrrolidine CAS NO 123-75-1, Pyrrolidine Suppliers, Pyrrolidine Manufacturers, related products of Pyrrolidine.
China CAS: 62613-82-5 Cp 99% White Powder Oxiracetam, Find details about China Oxiracetam, Testosterone Enanthate from CAS: 62613-82-5 Cp 99% White Powder Oxiracetam - Wuhan Yuancheng Gongchuang Technology Co., Ltd.
Prediction on the Inhibition Ratio of Pyrrolidine Derivatives on Matrix Metalloproteinase Based on Gene Expression Programming. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
A multivariate PLS-QSAR study with a data set of 31 cinnamoyl pyrrolidine derivatives described as type 2 matrix metalloproteinases (MMP-2) inhibitors is presented in this paper. The variable selection was performed with the Ordered Predictors Select
Abstract: The present invention relates to a new process for preparing 2-oxo-1-pyrrolidine derivatives of general formula (I), comprising the cyclisation of an intermediate of general formula (II) wherein the substituents are as defined in the specification. ##STR00001# ...
The effects of oxiracetam on hippocampally-mediated learning performance and hippocampal protein kinase C (PKC) were examined in C57BL/6Ibg (C57) and DBA/2Ibg (DBA) mice. C57 and DBA mice were subjected to daily injections of oxiracetam (50 mg/kg i.p.) or vehicle (0.9% saline) for a total of 9 days. …
The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. These compounds are synthesized from b-aryl pyrrolidines, providing products with the 2-arylethyl amine moiety, a structural feature often encountered in compounds active in the central nervous system. The b-aryl pyrrolidines are synthesized through a three-step methodology that includes a Knoevenagel condensation reaction, a 1,3-dipolar cycloaddition reaction, and a nitrile reduction.
What is the legal status of Oxiracetam for sale in Canada? Where can you purchase this racetam nootropic supplement over-the-counter in pill tablet or wholesale powder form? Information on ordering capsules from USA vendors, bulk prices and guide to Oxiracetam nootropic benefits, side effects and how to use for focus.
Oxiracetam is a nootropic in the racetam family. It is, like piracteam, water soluble. Oxiracetam is slightly more potent than piracetam, but significantly less
Highly functionalized pyrrolidines have gained much interest in the past few years as they constitute the main structural element of many natural and synthetic pharmacologically active compounds (Waldmann, 1995). Optically active pyrrolidines have been used as intermediates, chiral ligands or auxiliaries in controlled asymmetric synthesis (Suzuki et al., 1994; Huryn et al., 1991). In view of this importance, the crystal structure of the title compound has been carried out and the results are presented here.. The title compound consists of a pyrrolidine ring connected to a oxindole ring system at C1, a coumarine moiety at C2 and a benzene ring at C3. The X-ray analysis confirms the molecular structure and atom connectivity as illustrated in Fig.1.. The pyrrolidine (N1/C1-C4) ring adopts a twist conformation , with twist about the C4-N1 bond; the puckering parameters (Cremer & Pople, 1975), q2 = 0.4216 (14) Å and ϕ2 = 156.9 (2)°, and asymmetry parameters (Duax et al., 1976) ΔC2[C4-N1] = 5.0 ...
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Diabetes is often associated with psychological complications such as anxiety. The aim of this study was to evaluate the effects of pyrrolidine dithio..
ChemicalBook あなたのためにPYRROLIDINE-2-CARBOXYLIC ACID (4-METHOXY-PHENYL)-AMIDE(1163686-79-0)の化学的性質を提供して、融点、価格、蒸気圧、沸点、毒性、比重、沸点、密度、分子式、分子量、物理的な性質、毒性 税関のコードなどの情報、同時にあなたは更にPYRROLIDINE-2-CARBOXYLIC ACID (4-METHOXY-PHENYL)-AMIDE(1163686-79-0)の製品の全世界の供給商にブラウズすることができて、生産企業と生産メーカー、最後のPYRROLIDINE-2-CARBOXYLIC ACID (4-METHOXY-PHENYL)-AMIDE(1163686-79-0)の中国語、英文、用途 CAS cas number cas no可能性もあなたが必要とします。
Several 2-(aminomethyl)-and 2-(2-aminoethyl)-pyrrolidine-3,4-diol derivatives have been assayed for their inhibitory activities towards glycosidases. Good inhibitors of alpha-mannosidases must have the (2R,3R,4S) configuration and possess 2-(benzylamino)methyl substituents. Stereomers with the (2S,3R,4S) configuration are also competitive inhibitors of alpha-mannosidases, but less potent as they share the configuration of C(1), C(2), C(3) Of beta-D-mannosides rather than that Of alpha-D-mannosides. Interestingly, (2S,3R,4S)-2-{2-[(4-phenyl)phenylamino]ethyl}pyrrolidine-3,4-diol (12g) inhibits several enzymes, for instance alpha-L-fucosidase from bovine epididymis (K-i = 6.5 muM, competitive), alpha-galactosidase from bovine liver (K-i = 5 muM, mixed) and alpha-mannosidase from jack bean (K-i = 102 muM, mixed). Diamines such as (2R,3S,4R)-2-[2-(phenylamino) or 2-(benzylamino)ethyl]pyrrolidine-3,4-diol (ent-1 2a, ent-12b) inhibit P-glucosidase from almonds (K-i = 13-40 muM, competitive). (C) 2003 Elsevier
[150 Pages Report] Check for Discount on 2016 (S)-(+)-2-(Methoxymethyl)pyrrolidine (CAS 63126-47-6) Industry Market Report report by Prof Research. The Global and Chinese (S)-(+)-2-(Methoxymethyl)pyrrolidine Industry, 2011-...
Amidification of L-proline (3) with (+)-(R,R)-6 and (-)-(S,S)tartaric anhydride diacetate (7) gave N-substituted L-proline derivatives 8a,b, respectively. Acids 8a,b were transformed into diesters 9a,b with MeOH/HCl. Similar reactions with methyl (2S,4R)-4 and (2R,4S)-4-acetoxypipecolate (5) led to bicyclic lactams 14a,b and 15a. Compounds 8a,b were converted into N-(trihydroxybutyl)pyrrolidine derivatives 8c,d, 10a,b and 11a,b. Methyl (2S,4R)-20a and (2R,4S)-4-acetoxyN-[(2S,3S)-1,2,3-trihydroxybutyl]pipecolate (20b) were obtained by displacement of (-)-(2S,2S)-2-O-benzyl-3,4-O-isopropylidene-1-deoxy-1-iodothreitol (19) by 4 and 5. Compounds 20a,b were converted into (2S,4R,2S,2S)-21a and (2R,4S,2S,3S)-4-hydroxy-2-hydromethyl-N-(2-benzyloxy-3,4-isopropylidenedioxy)piperidine (21b) and finally into unprotected pentols 22a,b. Nonprotected (2S,2S,3S)-11a and (2S,2R,3R)-N-(1,2,3-trihydroxybutyl)prolinol (11b), as well as 22a,b, did not inhibit any of the 13 glycosidases assayed. However, a ...
Die Endothelin (ET)-Achse stellt ein potentielles Ziel für die Therapie des Mammakarzinoms dar. In dieser Arbeit wird der Einfluss des selektiven ETAR-Antagonisten Atrasentan (ABT-627) auf das Wachstum von Mammakarzinom-Xenografttumoren im Mausmodell untersucht. Zunächst wurden 40 Mäuse in 4 Therapiearmen nach s.c. Injektion von Mammakarzinomzellen (MCF-7) in die rechte Flanke mit 1)Atrasentan 2)Paclitaxel 3)einer Kombination und 4) Trägerlösung behandelt. In einer zweiten Versuchsreihe wurden insgesamt 16 Mäuse entweder mit Atrasentan oder Trägerlösung behandelt. Ergebnisse: Es zeigte sich eine signifikante Wachstumshemmung der Tumore durch die Atrasentan-Therapie im Vergleich zur Kontrollgruppe (p = 0,002). In der zweiten Versuchsreihe wurde bei der Hälfte der Mäuse ein Tumorwachstum verhindert. Diskussion: Wir schlussfolgern aus unseren Daten, dass durch selektive Hemmung von ETAR mittels Atrasentan das Wachstum ETAR-positiver Tumoren in vivo gehemmt werden kann. Introduction: The ...
Atrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer. It is also being investigated as a therapy for diabetic kidney disease. Atrasentan failed a phase 3 trial for prostate cancer in patients unresponsive to hormone therapy. A second trial confirmed this finding. It is an endothelin receptor antagonist selective for subtype A (ETA). While other drugs of this type (sitaxentan, ambrisentan) exploit the vasoconstrictive properties of endothelin and are mainly used for the treatment of pulmonary arterial hypertension, atrasentan blocks endothelin induced cell proliferation.[citation needed] In April 2014, de Zeeuw et al. showed that 0.75 mg and 1.25 mg of atrasentan reduced urinary albumin by 35 and 38% respectively with modest side effects. Patients also had decreased home blood pressures (but no change in office readings) decrease total cholesterol and LDL. Patients in the 1.25 mg dose group had increased weight ...
Pyrrolidine, 1-(1-oxopentadecyl)- | C19H37NO | CID 574639 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
123-75-1 - RWRDLPDLKQPQOW-UHFFFAOYSA-N - Pyrrolidine - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Vancouver-based Chinook Therapeutics Obtains Worldwide Rights from AbbVie to Atrasentan with Plans to Develop for the Treatment of Kidney Disease. Vancouver, BC, January 30, 2020--Chinook Therapeutics, Inc., a biotechnology company focused on developing precision medicines for kidney diseases, announced it has entered into a license agreement with AbbVie, a research-based global biopharmaceutical company, for worldwide, exclusive rights to atrasentan, an endothelin receptor antagonist.
Protocols for PET image acquisition and analysis have been published previously (Buckholtz et al., 2010a,b). All PET images were acquired using [18F]fallypride [(S)-N-[(1-allyl-2-pyrrolidinyl)methyl]-5-(3-[18F]fluoropropyl)-2,3-dimethoxybenzamide], a substituted benzamide with very high affinity to D2/D3 receptors (Mukherjee et al., 2005). The use of [18F]fallypride in the present context is critical in that, unlike other D2/D3 ligands, [18F]fallypride allows stable estimates of D2-like binding in both striatal and extrastriatal regions (Mukherjee et al., 2002; Christian et al., 2004). It thus provides a unique ability to simultaneously examine human DA function in both cortical and striatal areas involved in cost/benefit decision-making. Previous work has demonstrated good test-retest reliability of [18F]fallypride measurements of non-displaceable binding potential (BPND)-a computed estimate of the number of available D2/D3 receptors-in both striatal and prefrontal areas (Mukherjee et al., ...
4-pyrrolidin-1-ylbutanenitrile 35543-25-0 MSDS report, 4-pyrrolidin-1-ylbutanenitrile MSDS safety technical specifications search, 4-pyrrolidin-1-ylbutanenitrile safety information specifications ect.
(2S,5R)-5-(4-Aminophenyl)-1-[2-[[(2S)-3-(4-hydroxyphenyl)-2-sulfanylpropanoyl]amino]acetyl]pyrrolidine-2-carboxylic acid | C22H25N3O5S | CID 44322098 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
The main purpose of this study is to look at the effects (good or bad) that Atrasentan given alone and Atrasentan given with Zometa has on levels of bon
Lookchem Provide Cas No.1354025-59-4 Basic information: Properties,Safety Data,Sds and Other Datebase. We also Provide Trading Suppliers & Manufacture for 1354025-59-4 3-[((S)-2-AMino-propionyl)-cyclopropyl-aMino]-pyrrolidine-1-carboxylic acid tert-butyl ester.
1-(4-chlorobenzenesulfonyl)pyrrolidine-2-carboxylic acid; CAS Number: 73096-27-2; Linear Formula: C11H12ClNO4S; find Key Organics / BIONET-KEY001123936 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich
TY - JOUR. T1 - Exploratory synthetic studies of the α-methoxylation of amides via cuprous ion-promoted decomposition of o-diazobenzamides. AU - Han, Gyoonhee. AU - LaPorte, Matthew G.. AU - McIntosh, Mathias C.. AU - Weinreb, Steven M.. AU - Parvez, Masood. PY - 1996/12/27. Y1 - 1996/12/27. N2 - A convenient nonelectrochemical amide oxidation method has been developed. The process involves a cuprous ion-promoted decomposition of o-diazobenzamides like 4, generated in situ from the corresponding o-aminobenzamides, to give N-acyliminium ion intermediate 9 via a 1,5-H-atom transfer, followed by metal-catalyzed oxidation of the resulting α-amidyl radical. The transformation produces α-methoxybenzamides 15 in good yields. An attempt was made to apply this oxidation method to a total synthesis of the alkaloid (-)-anisomycin (16). Scalemic o-aminobenzamide pyrrolidine derivatives 18a/18b underwent oxidation to give α-methoxylated amide substrates 19a/19b, respectively, in good yields. However, ...
| 227931 | (S)-2-(Methoxymethyl)pyrrolidin-1-amine | SAMP | (S)-(-)-1-Amino-2-(methoxymethyl) pyrrolidine | 59983-39-0 | MFCD00064485 | C6H14N2O |
Find manufacturers and suppliers for 3-Pyrrolidin-1-yl-propionic acid hydrochloride, 76234-38-3. Synonyms: 3-(Pyrrolidin-1-yl)propanoic acid hydrochloride
You can download our 2017 product catalog in various formats, request to have a hard copy sent to you, or view our products online. ...
Die Universität zu Köln ist eine Exzellenzuniversität mit dem klassischen Fächerspektrum einer Volluniversität. Als eine der größen Hochschulen Europas arbeitet sie in Forschung und Lehre auch international auf höchstem Niveau.
L-Arginine which is unabsorbed in the small intestine, is converted by colonic bacteria to pyrrolidine in the large intestine (colon), and this is then partly absorbed and excreted unchanged in the urine (Asatoor et al, 1962).[1]. It can take 3 or more hours for food to reach the colon (this varies dramatically from person to person, and depends highly on other contents in the digestive system). For this reason excess L-arginine supplements will not normally begin to produce pyrrolidine until several hours have passed.. ...
1-[2-(5-Methoxy-1H-indol-3-yl)ethyl]pyrrolidin-2,5-dione/ACM363590481 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
Learn more about methyl-2-methyl-6-pyrrolidin-3-yl-pyrimidin-4-yl-amine-dihydrochloride. We enable science by offering product choice, services, process excellence and our people make it happen.
Learn more about 4-methyl-2-pyrrolidin-2-yl-6-trifluoromethyl-pyrimidine-hydrochloride. We enable science by offering product choice, services, process excellence and our people make it happen.
TY - JOUR. T1 - [ 123I]Epidepride neuroimaging of dopamine D 2/D 3 receptor in chronic MK-801-induced rat schizophrenia model. AU - Huang, Yuan Ruei. AU - Shih, Jun Ming. AU - Chang, Kang Wei. AU - Huang, Chieh. AU - Wu, Yu Lung. AU - Chen, Chia Chieh. PY - 2012/8/1. Y1 - 2012/8/1. N2 - Purpose: [ 123I]Epidepride is a radio-tracer with very high affinity for dopamine D 2/D 3 receptors in brain. The importance of alteration in dopamine D 2/D 3 receptor binding condition has been wildly verified in schizophrenia. In the present study we set up a rat schizophrenia model by chronic injection of a non-competitive NMDA receptor antagonist, MK-801, to examine if [ 123I]epidepride could be used to evaluate the alterations of dopamine D 2/D 3 receptor binding condition in specific brain regions. Method: Rats were given repeated injection of MK-801 (dissolved in saline, 0.3mg/kg) or saline for 1month. Afterwards, total distance traveled (cm) and social interaction changes were recorded. Radiochemical ...
In connection with on-going studies of spiro-pyrrolidine derivatives (Girgis et al. 2012; Moustafa et al. 2012), the title compound, (I), was synthesised and characterised crystallographically. These compounds have biological activity and the structure of the skeltal structure is well established (Kumar et al. 2008).. There are two spiro links in the molecule, Fig. 1, i) where the piperidine and pyrrolidine rings are connected at C1, and ii) where the pyrrolidine ring and indole residue are connected at C6. The phenyl-methyl-idene functional group is connected to the piperidine ring at position C4 while the pyrrolidine-bound aryl ring is attached at C8. The conformation about the C4═C11 double bond is E. The sum of the angles around the piperidine-N1 atom is approximately 333° confirming its sp3 character. The piperidine ring adopts a half-chair conformation where the C2 atom lies 0.713 (3) Å out of the plane of the remaining five atoms (r.m.s. deviation = 0.086 Å). The C6 and C8 atoms ...
0066] Specific examples of the compound (I) of the present invention include: [0067] 7-[(3S,4S)-3-amino-4-ethylpyrrolidin-1-yl]-6-fluoro-1-[(1R,2S)-2-(S)-fluo- rocyclopropyl]-1,4-dihydro-8-methoxy-4-oxoquinoline-3-carboxylic acid, a salt, or a hydrate thereof (Compound No. 1); [0068] 7-[(3S,4S)-3-amino-4-ethylpyrrolidin-1-yl]-6-fluoro-1-[(1R,2S)-2-fluorocy- clopropyl]-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid, a salt, or a hydrate thereof (Compound No. 2); [0069] (3S)-10-[(3S,4S)-3-amino-4-ethylpyrrolidin-1-yl]-9-fluoro-2,3-dihydro-3-m- ethyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid, a salt, or a hydrate thereof (Compound No. 3); [0070] 7-[(3S,4S)-3-amino-4-propylpyrrolidin-1-yl]-6-fluoro-1-[(1R,2S)-2-fluoroc- yclopropyl]-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid, a salt, or a hydrate thereof (Compound No. 4); [0071] 7-[(3S,4S)-3-amino-4-propylpyrrolidin-1-yl]-6-fluoro-1-[(1R,2S)-2-fluoroc- yclopropyl]-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic ...
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This study investigated whether D,L-cis-2,3-Pyrrolidine dicarboxylate (D,L-cis-2,3-PDC), a new glutamate analogue, alters glutamate binding to cerebral plasma membranes and whether N-methyl-D-aspartate (NMDA) receptors are involved in the convulsant effect of this compound. D,L-cis-2,3-PDC reduced sodium-independent [3H]-L-glutamate binding to lysed membrane preparations from adult rat cortex and had no effect on sodium-dependent glutamate binding. Intracerebroventricular administration of D,L-cis-2,3-PDC (7.5-25 nmol/5 microl) induced generalized tonic-clonic convulsions in mice in a dose-dependent manner. The coadministration of MK-801 (7 nmol/2.5 microl), with D,L-cis-2,3-PDC (16.5 nmol/2.5 microl), fully protected the animals against D,L-cis-2,3-PDC-induced convulsions, while the coadministration of DNQX (10 nmol/2.5 microl) increased the latency to convulsions but did not alter the percentage of animals that had convulsions. These results suggest that D,L-cis-2,3-PDC-induced effects are mediated
(3-Pyrrolidin-1-ylphenyl)methanol, 97%, Maybridge 250mg (3-Pyrrolidin-1-ylphenyl)methanol, 97%, Maybridge Pyrimidj to Pz -Organics
Making waste a functionality: Oxidative electron transfer-mediated anion-radical transformations are rendered catalytic by employing a 2,2,6,6-tetramethyl-N-oxopiperidinium salt with ferrocene. This enables an asymmetric approach to highly functionalized cyclopentane and pyrrolidine derivatives. At the same time the co-generated reduced species TEMPO serves as a useful oxygenating functionality. ...
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1 Click Chemistry Suppliers ,1461707-59-4,1-(4-fluorobenzoyl)pyrrolidin-3-amine hydrochloride,Cl.FC1=CC=C(C=C1)C(=O)N2CC(N)CC2,C11H13N2OF.HCl,MFCD25371661,1-(4-fluorobenzoyl)pyrrolidin-3-amine hydrochloridefor your research needs
SWISS-MODEL Template Library (SMTL) entry for 1ivp.1. THE CRYSTALLOGRAPHIC STRUCTURE OF THE PROTEASE FROM HUMAN IMMUNODEFICIENCY VIRUS TYPE 2 WITH TWO SYNTHETIC PEPTIDIC TRANSITION STATE ANALOG INHIBITORS
2jff: Structural and functional characterization of enantiomeric glutamic acid derivatives as potential transition state analogue inhibitors of MurD ligase.
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Product: [1-(3-Chloro-5-trifluoromethyl-pyridin-2-yl)-pyrrolidin-2-yl]-methanol CAS: 1306120-26-2 Purity: Commodity Code:2933998090 MDL Number:MFCD13484412 Synonyms:
Founded in 2011, Suzhou Xinkai Bio-Medical Technology Co., Ltd. is located in Suzhou New District of Suzhou city in Jiangsu province. Xinkai focus is on the development of...
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Serradeil-Le Gal C, Wagnon J, Simiand J, Griebel G, Lacour C, Guillon G, Barberis C, Brossard G, Soubrié P, Nisato D, Pascal M, Pruss R, Scatton B, Maffrand JP, Le Fur G (2002). „Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist. J. Pharmacol. Exp. Ther. 300 (3): 1122-30. PMID 11861823. doi:10.1124/jpet.300.3.1122 ...
Anisomycin is a pyrrolidine antibiotic, acts as an anti-fungal antibiotic which inhibits Protein Synthesis, also is a potent activator of SAPKs/JNKs. ...Quality confirmed by NMR,HPLC & MS.
I. R. Laskar, T. K. Maji, D. Das, T.-H. Lu, W.-T. Wong, K. Okamoto and N. Ray Chaudhuri, Syntheses, characterization and solid state thermal studies of 1-(2-aminoethyl)piperidine (L), 1-(2-aminoethyl) pyrrolidine (L) and 4-(2-aminoethyl)morpholine (L) complexes of nickel(II): X-ray single crystal structure analyses of trans-[NiL2(CH3CN)2](ClO4)2, trans-[NiL2(NCS)2] and trans-[NiL2(NCS)2], Polyhedron 20, 2073 (2001 ...
0198]In any of the reactions mentioned hereinbefore and hereinafter, protecting groups may be used where appropriate or desired, even if this is not mentioned specifically, to protect functional groups that are not intended to take part in a given reaction, and they can be introduced and/or removed at appropriate or desired stages. Reactions comprising the use of protecting groups are therefore included as possible wherever reactions without specific mentioning of protection and/or deprotection are described in this specification. Within the scope of this disclosure only a readily removable group that is not a constituent of the particular desired end product of formula XIV is designated a protecting group, unless the context indicates otherwise. The protection of functional groups by such protecting groups, the protecting groups themselves, and the reactions appropriate for their introduction and removal are described for example in standard reference works, such as J. F. W. McOmie, ...
Product Number: C5851 CAS number: 273404-37-8 Synonyms: VX-765, (2S)-1-[(2S)-2-[(4-Amino-3-chlorobenzoyl)amino]-3,3-dimethylbutanoyl]-N-[(2R,3S)-2-ethoxy-5-oxooxolan-3-yl]pyrrolidine-2-carboxamide. ...
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In case of thermal initiation, the N-chloroamines give better yields for pyrrolidines because N-bromoamines are less stable ... In contrast, when the initiation is carried out by irradiation, the N-bromoamines give higher yield for pyrrolidines.[failed ... The formation of the pyrrolidine ring of 40 was accomplished by irradiation of N-chloroamide 39. Another variation of the ... The most prevalent synthetic utility of the Hofmann-Löffler-Freytag reaction is the assembly of the pyrrolidine ring. The ...
Pipradrol Pyrrolidines: Diphenylprolinol • Methylenedioxypyrovalerone (MDPV) • Naphyrone • Prolintane • Pyrovalerone Tropanes: ...
... , also known as (-)-3β-(4-iodophenyl)tropane-2β-pyrrolidine carboxamide and RTI-4229-229, is a potent and long-lasting ... tropane-2β-pyrrolidine carboxamide ([125I]RTI-229)". Journal of Labelled Compounds and Radiopharmaceuticals. 42 (3): 281-286. ... iodophenyl group at the 3β-position and a pyrrolidine carboxamide at 2β, RTI-229 has extremely high selectivity for the ...
3-amino-pyrrolidine and benzylamine templates.[35] ...
... emerged as a new legal high in the United Kingdom only months after the ban of similar drug mephedrone (which was also a cathinone derivative). Until July 2010 the substance was not controlled by the Misuse of Drugs Act 1971 and was therefore not illegal for someone to possess. The Medicines Act prevented naphyrone from being sold for human consumption, and therefore it was sometimes sold as 'pond cleaner' or as another substance not normally consumed by humans. In response to this emerging trend of new designer drugs, Home Office Minister James Brokenshire said, "action to address the issue of emerging legal highs coming on to the market is a priority for the government."[12][unreliable source?] A study by researchers at Liverpool John Moores University found that only one out of ten products labelled as "NRG-1" actually contained naphyrone when they were subjected to laboratory analysis. Compounds found in products labelled NRG-1 included MDPV, flephedrone, mephedrone, butylone and ...
... is a synthetic form of the isolated major active metabolite of venlafaxine, and is categorized as a serotonin-norepinephrine reuptake inhibitor (SNRI). When most normal metabolizers take venlafaxine, approximately 70% of the dose is metabolized into desvenlafaxine, so the effects of the two drugs are expected to be very similar.[5] It works by blocking the "reuptake" transporters for key neurotransmitters affecting mood, thereby leaving more active neurotransmitters in the synapse. The neurotransmitters affected are serotonin (5-hydroxytryptamine) and norepinephrine (noradrenaline). It is approximately 10 times more potent at inhibiting serotonin uptake than norepinephrine uptake.[6]. ...
... was discovered by scientists at Angelini, who also discovered trazodone.[15] Its development names have included ST-1191 and McN-A-2673-11.[16][1] The INN etoperidone was proposed in 1976 and recommended in 1977.[17][18] The drug was given brand names in Spain (Centren (Esteve) and Depraser (Lepori)) and Italy (Staff (Sigma Tau))[1] and was also given the brand names Axiomin and Etonin,[16] but it is not entirely clear if it was actually marketed; the Pharmaceutical Manufacturing Encyclopedia provides no dates for commercial introduction.[19] According to Micromedex's Index Nominum: International Drug Directory, etoperidone was indeed previously marketed in Spain and Italy.[1] ...
McConathy J, Owens MJ, Kilts CD, et al. (August 2004). "Synthesis and biological evaluation of [11C]talopram and [11C]talsupram: candidate PET ligands for the norepinephrine transporter". Nuclear Medicine and Biology. 31 (6): 705-18. doi:10.1016/j.nucmedbio.2003.05.001. PMID 15246361 ...
The mechanism of action of armodafinil is unknown. Armodafinil (R-(−)-modafinil) has pharmacological properties almost identical to those of modafinil (a mixture of R-(−)- and (S)-(+)-modafinil). The (R)- and (S)-enantiomers have similar pharmacological action in animals. Armodafinil has wake-promoting actions similar to sympathomimetic agents including amphetamine and methylphenidate, although its pharmacologic profile is not identical to that of the sympathomimetic amines. Armodafinil is an indirect dopamine receptor agonist; it binds in vitro to the dopamine transporter (DAT) and inhibits dopamine reuptake. For modafinil, this activity has been associated in vivo with increased extracellular dopamine levels. In genetically engineered mice lacking the dopamine transporter, modafinil lacked wake-promoting activity, suggesting that this activity was DAT-dependent. However, the wake-promoting effects of modafinil, unlike those of amphetamine, were not antagonized by the dopamine receptor ...
... or WF-23 is a cocaine analogue. It is claimed to be several hundred times more potent than cocaine at being a serotonin-norepinephrine-dopamine reuptake inhibitor.[1] As can be seen on pubmed, these acyl substituted phenyltropanes are highly potent MAT inhibitors and also have a very long half-life, spanning perhaps at least a few days.[2] [3] ...
"Pharmaceutical compositions and methods for treating compulsive disorders using pyrrolidine derivatives" ...
MDPV undergoes CYP450 2D6, 2C19, 1A2,[17] and COMT phase 1 metabolism (liver) into methylcatechol and pyrrolidine, which in ... Hydroxylation of both the aromatic ring and side chain then takes place, followed by an oxidation of the pyrrolidine ring to ... These impurities likely account for its discoloration and fishy (pyrrolidine) or bromine-like odor, which worsens upon exposure ... Impurities are likely to consist of either pyrrolidine or alpha-dibrominated alkylphenones-respectively, from either excess ...
... (CGP-15,210-G) is a selective serotonin reuptake inhibitor (SSRI) which was investigated as an antidepressant in the 1980s but was never marketed.[1][2][3] Ifoxetine selectively blocks the reuptake of serotonin in the brain supposedly without affecting it in the periphery.[3] Supporting this claim, ifoxetine was found to be efficacious in clinical trials and was very well tolerated, producing almost no physical side effects or other complaints of significant concern.[3] ...
... is a norepinephrine-dopamine reuptake inhibitor (NDRI) under development by Jazz Pharmaceuticals for the treatment of excessive sleepiness associated with narcolepsy and sleep apnea. It is derived from phenylalanine and its chemical name is (R)-2-amino-3-phenylpropylcarbamate hydrochloride.[1] The drug was discovered by a subsidiary of SK Group, which licensed rights outside of 11 countries in Asia to Aerial Pharma in 2011.[2] Aerial ran two Phase II trials of the drug in narcolepsy[3] before selling the license to solriamfetol to Jazz in 2014; Jazz paid Aerial $125 million up front and will pay Aerial and SK up to $272 million in milestone payments, and will pay double digit royalties to SK.[2][4] Solriamfetol had also been tested in animal models of depression, but as of 2017 that work had not been advanced to clinical trials.[5] During development it has been called SKL-N05, ADX-N05, ARL-N05, and JZP-110.[6] In March 2018 the FDA accepted SK's and Jazz' NDA for use of ...
InChI=1S/C32H38N2O8/c1-37-24-12-17(13-25(38-2)29(24)39-3)31(35)42-26-14-18-16-34-11-10-20-19-8-6-7-9-22(19)33-28(20)23(34)15-21(18)27(30(26)40-4)32(36)41-5/h6-9,12-13,18,21,23,26-27,30,33H,10-11,14-16H2,1-5H3/t18-,21+,23-,26-,27+,30+/m1/s1 ...
Pyrrolidines. *Serotonin-norepinephrine-dopamine reuptake inhibitors. Hidden categories: *Articles with changed EBI identifier ...
Starr KR, Price GW, Watson JM, Atkinson PJ, Arban R, Melotto S, Dawson LA, Hagan JJ, Upton N, Duxon MS (2007). "SB-649915-B, a novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor, is anxiolytic and displays fast onset activity in the rat high light social interaction test". Neuropsychopharmacology. 32 (10): 2163-2172. doi:10.1038/sj.npp.1301341. PMID 17356576 ...
... (Merital, Alival) is a norepinephrine-dopamine reuptake inhibitor, i.e. a drug that increases the amount of synaptic norepinephrine and dopamine available to receptors by blocking the dopamine and norepinephrine reuptake transporters.[2] This is a mechanism of action shared by some recreational drugs like cocaine and the medication tametraline (see DRI). Research showed that the (S)-isomer is responsible for activity.[3] The drug was developed in the 1960s by Hoechst AG (now Sanofi-Aventis),[4] who then test marketed it in the United States. It was an effective antidepressant, without sedative effects. Nomifensine did not interact significantly with alcohol and lacked anticholinergic effects. No withdrawal symptoms were seen after 6 months treatment. The drug was however considered not suitable for agitated patients as it presumably made agitation worse.[5][6] In January 1986 the drug was withdrawn by its manufacturers for safety reasons.[7] Some case reports in the 1980s suggested ...
... (developmental code names SL 81-0385, IXA-001) is an antidepressant which was under clinical development for the treatment of depression in the early 1990s but was never marketed.[1][2] It acts as a potent serotonin reuptake inhibitor (Ki for SERT = 7 nM) and modest 5-HT3 receptor antagonist (Ki = 315 nM).[3][4] It has antiemetic activity, and unlike the selective serotonin reuptake inhibitors (SSRIs), appears to have a negligible incidence of nausea and vomiting.[5] The drug is structurally related to indalpine.[4] Development of litoxetine for depression was apparently ceased in the late 1990s.[6] However, as of March 2017, development of litoxetine has been reinitiated and the drug is now in the phase II stage for the treatment of urinary incontinence.[6] ...
... (brand names Sidnocarb, Sydnocarb) is a drug that is currently being developed for Parkinson's disease.[1] The drug was originally developed in the USSR in the 1970s [2][3] for a variety of indications including asthenia, apathy, adynamia and some clinical aspects of depression and schizophrenia.[4][5] Mesocarb was used for counteracting the sedative effects of benzodiazepine drugs,[6] increasing workload capacity and cardiovascular function,[7] treatment of ADHD and hyperactivity in children,[8][9] as a nootropic,[10] and as a drug to enhance resistance to extremely cold temperatures.[11][12] It is also listed as having antidepressant and anticonvulsant properties. The drug has been found to act as a selective dopamine reuptake inhibitor by blocking the actions of the dopamine transporter (DAT),[13][14] and lacks the dopamine release characteristic of stimulants such as dextroamphetamine.[15][16][17] It was the most selective DAT inhibitor amongst an array of other DAT inhibitors to ...
Randomized, double blind, placebo-controlled trials have confirmed the efficacy of dapoxetine for the treatment of PE.[8] Different dosage has different impacts on different types of PE. Dapoxetine 60 mg significantly improves the mean intravaginal ejaculation latency time (IELT) compared to that of dapoxetine 30 mg in men with lifelong PE, but there is no difference in men with acquired PE.[9] Dapoxetine, given 1-3 hours before sexual episode, prolongs IELT and increases the sense of control and sexual satisfaction in men of 18 to 64 years of age with PE. Since PE is associated with personal distress and interrelationship difficulty, dapoxetine provides help for men with PE to overcome this condition.[10] With no drug approved specifically for treatment for PE in the US and some other countries, other SSRIs such as fluoxetine, paroxetine, sertraline, fluvoxamine, and citalopram have been used off-label to treat PE. Waldinger's meta-analysis shows that the use of these conventional ...
... may be synthesized in a straightforward fashion via the Diels-Alder reaction between cyclopentadiene and β-nitrostyrene (1-nitro-2-phenyl-ethene). The C=C double bond and the nitro-group in the resulting norcamphene derivative are then reduced to give the saturated norcamphane derivative. Finally, the amino-group is ethylated. Although β-nitrostyrene is commercially available, it is also very easily prepared using the Henry Reaction between benzaldehyde and nitromethane.[7] The Diels-Alder reaction of β-nitrostyrene and cyclopentadiene is described in a number of early papers.[8][9] The reduction of the nitroalkene may be carried out sequentially. The alkene's double bond is typically reduced using hydrogen and a transition metal catalyst like Ni or Pt, while the nitro group is reduced to the amine with a metal/acid combination, such as Fe/HCl.[9] The reduction of both functional groups can also be achieved simultaneously by the use of Raney nickel,[9] and this transformation has ...
There has been much debate as to whether reboxetine is more efficacious than placebo in the treatment of depression. According to a 2009 meta-analysis of 12 second-generation antidepressants, reboxetine was no more effective than placebo, and was "significantly less" effective, and less acceptable, than the other drugs in treating the acute-phase of adults with unipolar major depression.[5] The British MHRA said in September 2011 that the study had several limitations, and that "Overall the balance of benefits and risks for reboxetine remains positive in its authorised indication."[6] A UK and Europe-wide review of available efficacy and safety data has confirmed that reboxetine has benefit over placebo in its authorised indication. Efficacy was clearly shown in patients with severe or very severe depression.[6] According to a systematic review and meta-analysis by IQWiG, including unpublished data, published data on reboxetine overestimated the benefit of reboxetine versus placebo by up to 115% ...
Pyrrolidines. *2-Diphenylmethylpyrrolidine. *4-Cl-PVP. *5-DBFPV. *α-PPP. *α-PBP ...
... , sold under the brand name Azafen or Azaphen, is an antidepressant approved in Russia for the treatment of depression.[1][2][3][4] It was introduced in the late 1960s and is still used today.[5][6] Pipofezine has been shown to act as a potent inhibitor of the reuptake of serotonin.[7][8] In addition to its antidepressant action, pipofezine has sedative effects as well, suggesting antihistamine activity.[4] Other properties such as anticholinergic or antiadrenergic actions are less clear but are likely.[citation needed] ...
Sakamuri, S.; Enyedy, I. J.; Zaman, W. A.; Tella, S. R.; Kozikowski, A. P.; Flippen-Anderson, J. L.; Farkas, T.; Johnson, K. M.; Wang, S. (2003). "2,3-Disubstituted quinuclidines as a novel class of dopamine transporter inhibitors". Bioorganic & Medicinal Chemistry. 11 (6): 1123-1136. doi:10.1016/S0968-0896(02)00450-9. PMID 12614900 ...
... is effective for prevention of shivering during surgery or recovery from surgery.[5][6] Nefopam was significantly more effective than aspirin as an analgesic in one clinical trial,[7] although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses.[8][9] The estimated relative potency of nefopam to morphine indicates that 20 mg of nefopam HCl is the approximate analgesic equal of 12 mg of morphine with comparable analgesic efficacy to morphine,[10][11][12] or oxycodone,[13] while Nefopam tends to produce fewer side effects, does not produce respiratory depression,[14] and has much less abuse potential, and so is useful either as an alternative to opioids, or as an adjunctive treatment for use alongside opioid(s) or other analgesics.[12][15] Nefopam is also used to treat severe hiccups.[16] ...
Common side effects include drowsiness, dry mouth, loss of appetite, sweating, trouble sleeping, and sexual dysfunction.[5] Serious side effects may include suicide in those under the age of 25, serotonin syndrome, and mania.[5] While rate of side effects appear similar compared to other SSRIs and SNRIs, antidepressant discontinuation syndromes may occur more often.[39][40] Use in pregnancy is not recommended while use during breastfeeding is relatively safe.[9] Paroxetine shares many of the common adverse effects of SSRIs, including (with the corresponding rates seen in people treated with placebo in parentheses): nausea 26% (9%), diarrhea 12% (8%), constipation 14% (9%), dry mouth 18% (12%), somnolence 23% (9%), insomnia 13% (6%), headache 18% (17%), hypomania 1% (0.3%), blurred vision 4%(1%), loss of appetite 6% (2%), nervousness 5% (3%), paraesthesia 4% (2%), dizziness 13% (6%), asthenia (weakness; 15% (6%)), tremor 8% (2%), sweating 11% (2%), and sexual dysfunction (≥10% incidence).[4] ...
... is a stimulant drug which acts as a norepinephrine-dopamine reuptake inhibitor, structurally related to the better known drug fencamfamine.[1][2][3] It was developed by the pharmaceutical company Eli Lilly in the 1970s, and researched for potential use as an antidepressant, although never marketed. LR-5182 has two stereoisomers, both of which are active, although one isomer blocks reuptake of only dopamine and noradrenaline, while the other blocks reuptake of serotonin as well.[4] While LR-5182 itself never proceeded beyond initial animal studies, discovery of monoamine reuptake inhibition activity and stimulant effects in drugs of this type has subsequently led to the development of many other stimulant drugs of related chemical structure, primarily developed as potential antidepressants,[5] or as substitute drugs for the treatment of cocaine abuse.[6][7] LR-5659 is planar and contains a Bicyclo-octene. This itself is fully active: DA 9nM, NE 27nM, SER 0.6 μM. ...
A New Pyrrolidine Synthesis". J. Am. Chem. Soc. 101 (5): 1310-1312. doi:10.1021/ja00499a058. Overman L.E.; Kakimoto M.; Okawara ... The aza-Cope/Mannich reaction is often the most efficient way to synthesize pyrrolidine rings, and thus has a number of ... This synthesis is one example of many of the cyanomethyl group providing a synthetically useful route towards pyrrolidine and ... Other routes toward pyrrolidine synthesis cannot compete with the stereospecificity, widescale applications in structures ...
Pyrrolidine is a base. Its basicity is typical of other dialkyl amines. Relative to many secondary amines, pyrrolidine is ... many substituted pyrrolidines are known. Pyrrolidine is prepared industrially by the reaction of 1,4-butanediol and ammonia at ... Many modifications of pyrrolidine are found in natural and synthetic chemistry. The pyrrolidine ring structure is present in ... Pyrrolidine is used as a building block in the synthesis of more complex organic compounds. It is used to activate ketones and ...
Pyrrolidine dithiocarbamate is jargon for various salts containing the pyrrolidine dithiocarbamate anion C4H8NS2−. ... Pyrrolidine dithiocarbamate (PDTC) is are a family of closely related drugs used for a metal chelation, induction of G1 phase ... Pyrrolidine dithiocarbamate binds zinc such that the resulting complex can enter the cell and inhibit viral RNA-dependent RNA ...
Learn More about Pyrrolidines
pyrrolidines.html >Pyrrolidines
pyrrolidine ring is the central structure of the amino acid proline and its derivatives. Chiral pyrrolidines play an ... A href=/technical-documents/articles/chemfiles/chiral-pyrrolidines.html >Chiral Pyrrolidines
pyrrolidines as heterocyclic building blocks for organic synthesis and medicinal ...
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
Other names: N-Acetylpyrrolidine; 1-Acetylpyrrolidine; N-Acetypyrrolidine; Pyrrolidine, N-acetyl; Acetylpyrrolidine; Ethanone, ...
This project is supported by the Canadian Institutes of Health Research (award #111062), Alberta Innovates - Health Solutions, and by The Metabolomics Innovation Centre (TMIC), a nationally-funded research and core facility that supports a wide range of cutting-edge metabolomic studies. TMIC is funded by Genome Alberta, Genome British Columbia, and Genome Canada, a not-for-profit organization that is leading Canadas national genomics strategy with funding from the federal government. Maintenance, support, and commercial licensing is provided by OMx Personal Health Analytics, Inc. Designed by Educe Design & Innovation Inc. ...
... Xiuli Chang, Chunfeng Shao, Qing Wu, Qiangen Wu, ... A. Iseki, F. Kambe, K. Okumura et al., "Pyrrolidine dithiocarbamate inhibits TNF-. a. -dependent activation of NF-. ?. B by ... Pyrrolidine dithiocarbamate (. 99%) was purchased from Sigma-Aldrich (St. Louis, Mo, USA). 45% paraquat concentration was ... B activation by pyrrolidine dithiocarbamate prevents in vivo expression of proinflammatory genes," Circulation, vol. 100, no. ...
... pyrrolidine 0.97; CAS No.: 132883-44-4; Synonyms: (3S)-N,N-Dimethyl-3-pyrrolidinamine; Linear Formula: C6H14N2; Empirical ... S)-(−)-3-(Dimethylamino)pyrrolidine 97% Synonym: (3S)-N,N-. Dimethyl-. 3-. pyrrolidinamine ...
For example, 3-amino-2-oxo-pyrrolidines are preferably used as a structural unit for peptide mimetics, which are used as ... 50 g (0.15 mol) of 3-benzyloxycarbonyl-amino-1-(4-cyanophenyl)-2-oxo-pyrrolidine are suspended in 600 ml of methanol, and 14.1 ... In WO 94/22820, 3-amino-1-phenyl-2-oxo-pyrrolidines substituted at the phenyl ring, for example, are described as intermediates ... The majority of the processes used hitherto for the preparation of substituted 3-amino-2-oxo-pyrrolidines consist in first ...
3S)-(-)-3-(Trifluoroacetamido)pyrrolidine Hydrochloride 98.0 %, TCI America 1G Chemicals:Organic Compounds:Organic salts: ...
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development ... NVP-DPP728 (1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano-(S)- pyrrolidine), a slow-binding inhibitor of ... The pyrrolidine alkaloid, 2,5-dihydroxymethyl-3,4-dihydroxypyrrolidine, inhibits glycoprotein processing. Elbein, A.D., ... Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally ...
A series of arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines was synthesized to develop new α1- ... Arylsulfonamide derivatives of pyrrolidines and piperidines; Benign prostatic hyperplasia; LCAP flexible biomimetic; ... Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α1-adrenergic receptor antagonist with uro- ...
... pyrrolidines and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R,sub,1,/ ... pyrrolidine 530.2. 3 d1 + d2. N-methylpiperazine. 559.3. 4 d1 + d2. piperidine 544.3. 5 d1 + d2. ethanolamine 520.2. 6 d1 + d2 ... pyrrolidine 521.3. 3 d1 N-methylpiperazine. 550.4. 4 d2 N-methylpiperazine. 550.4. 5 d1 + d2. piperidine 535.4. 6 d1 + d2. ... When n is 1, a pyrrolidine ring is formed, when n is 2 a piperidine ring is formed, and when n is 3 the ring is designated as a ...
1-pyrrolidineethanol, n-2-hydroxyethyl pyrrolidine, 1-2-hydroxyethyl pyrrolidine, 2-pyrrolidin-1-yl ethanol, epolamine, 2- ... 1-pyrrolidineethanol, n-2-hydroxyethyl pyrrolidine, 1-2-hydroxyethyl pyrrolidine, 2-pyrrolidin-1-yl ethanol, epolamine, 2- ...
N,N-(3S,4S)-pyrrolidine-3,4-diylbis[N-(4-iodobenzyl)benzenesulfonamide]. C30 H29 I2 N3 O4 S2. ALNICVDMFYPVLU-KYJUHHDHSA-N. ... Structure-Guided Design of C2-Symmetric HIV-1 Protease Inhibitors Based on a Pyrrolidine Scaffold.. Blum, A., Bottcher, J., ... By use of pyrrolidine as core structure, symmetric 3,4-bis-N-alkylsulfonamides were designed and synthesized enantioselectively ... HIV-1 Protease in complex with a iodo decorated pyrrolidine-based inhibitor. *DOI: 10.2210/pdb2QNP/pdb ...
... pyrrolidine-2-carboxylic acid
Precautionary Statements: P280-P303+P361+P353-P305+P351+P338-P310a Wear protective gloves/protective clothing/eye protection/face protection. IF ON SKIN (or hair): Remove/Take off immediately all contaminated clothing. Rinse skin with water/shower. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. Immediately call a POISON CENTER/doctor ...
Pyrrolidine-2-carbonylamino)acetyl]amino]acetic acid , C9H15N3O4 , CID 263466 - structure, chemical names, physical and ...
X. Li and J. Li, "Recent advances in the development of MMPIs and APNIs based on the pyrrolidine platforms," Mini-Reviews in ... X.-C. Cheng, Q. Wang, H. Fang, and W.-F. Xu, "Advances in matrix metalloproteinase inhibitors based on pyrrolidine scaffold," ... L. Zhang, W.-F. Xu, and J. Zhang, "Protein catabolic enzymes inhibitory activities of pyrrolidine derivatives," Chinese ...
... pyrrolidine-2-carboxylic acid , C17H17NO3 , CID 20542584 - structure, chemical names, physical and chemical properties, ...
We also Provide Trading Suppliers & Manufacture for 1270491-62-7 2-(3-Ethoxyphenyl)pyrrolidine. ... 2-(3-ethoxyphenyl)pyrrolidine. Cas No: 1270491-62-7. No Data. No Data. No Data. Health Chemicals Co., Ltd.. Contact Supplier ... CAS DataBase Reference: 2-(3-Ethoxyphenyl)pyrrolidine(CAS DataBase Reference). *NIST Chemistry Reference: 2-(3-Ethoxyphenyl) ...
3,4-dihydroxy-1-[(Z)-octadec-9-enyl]pyrrolidine-2,5-dione. Regulatory process names 1 IUPAC names 1 ...
The b-aryl pyrrolidines are synthesized through a three-step methodology that includes a Knoevenagel condensation reaction, a 1 ... These compounds are synthesized from b-aryl pyrrolidines, providing products with the 2-arylethyl amine moiety, a structural ... The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. ... The b-aryl pyrrolidines are synthesized through a three-step methodology that includes a Knoevenagel condensation reaction, a 1 ...
For the bioactivity of pyrrolidine-2,5-dione derivatives, see: Obniska et al. (2012. ); Ha et al. (2011. ); Kaminski et al. ( ... For the bioactivity of pyrrolidine-2,5-dione derivatives, see: Obniska et al. (2012); Ha et al. (2011); Kaminski et al. (2011 ... In the title compound, C13H15NO3, the pyrrolidine ring makes a dihedral angle of 4.69 (9)° with the 3-meth-oxy-phenyl ring. In ... 1, the pyrrolidine ring (N1/C10-C13) makes a dihedral angle of 4.69 (9)° with the benzene ring (C2-C7). ...
For pyrrolidine properties, see: Chen et al. (2012. ); Boyd et al. (1999. ). For tandem reactions under radical conditions, see ... In the title compound, C21H22N2O, the planes of the two six-membered rings make a dihedral angle of 89.51 (7)°. The pyrrolidine ... The title compound, 1-(benzyloxy)-5-cyanomethyl-2,3-dihydrospiro [inden-1,2-pyrrolidine], (trans-IIIa), belongs to the ... 2-[1′-(Benz-yl-oxy)spiro-[indane-1,2′-pyrrolidine]-5′-yl]aceto-nitrile. ...
Dichiarazioni precauzionali: P261-P280a-P305+P351+P338-P304+P340-P405-P501a Avoid breathing dust/fume/gas/mist/vapours/spray. Wear protective gloves and eye/face protection. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. IF INHALED: Remove to fresh air and keep at rest in a position comfortable for breathing. Store locked up. Dispose of contents/container in accordance with local/regional/national/international regulations. ...
This page contains information on the chemical Pyrrolidine, 1-((1-(2-benzylphenoxy)methyl)ethyl)-, hydrogen phosphate including ... 1-((1-(2-Benzylphenoxy) methyl) ethyl) pyrrolidine hydrogen phosphate*Pyrrolidine, 1-((1-(2-benzylphenoxy) methyl) ethyl)-, ... Pyrrolidine, 1-((1-(2-benzylphenoxy) methyl) ethyl)-, hydrogen phosphate. Identifications. *CAS Number: 10429-40-0*Synonyms/ ... Chemical Database - Pyrrolidine, 1-((1-(2-benzylphenoxy)methyl)ethyl)-, hydrogen phosphate. EnvironmentalChemistry.com. 1995 - ...
The aim of this study was to evaluate the effects of pyrrolidine dithio.. ... Pyrrolidine Dithiocarbamate Alleviated Anxiety in Diabetic Mice. Author(s): C. Guangpin, L. Chuntao, Q. Ping, H. Yue and M. ... In conclusion, pyrrolidine dithiocarbamate treatment in diabetic mice exerted anxiolytic-like effects. The present study might ... Confirmed diabetic mice (,16.7 mM/l of blood glucose) were treated with pyrrolidine dithiocarbamate or 0.9% saline for 10 w. ...
A series of trans-N-alkyl-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanemethylamines was synthesized and ... Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for ...
Market Research Report 2019 aims at providing comprehensive data on n-methyl pyrrolidine market globally and regionally ... N-methyl pyrrolidine prices in other regions. 7. N-METHYL PYRROLIDINE END-USE SECTOR 7.1. N-methyl pyrrolidine market by ... N-methyl pyrrolidine market forecast. 6. N-METHYL PYRROLIDINE MARKET PRICES. 6.1. N-methyl pyrrolidine prices in Europe. 6.2. N ... 3. N-METHYL PYRROLIDINE MANUFACTURING METHODS. 4. N-METHYL PYRROLIDINE PATENTS. Abstract. Description. Summary of the invention ...
  • The amino acids proline and hydroxyproline are, in a structural sense, derivatives of pyrrolidine. (wikipedia.org)
  • The pyrrolidine ring is the central structure of the amino acid proline and its derivatives. (sigmaaldrich.com)
  • Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α1-adrenergic receptor antagonist with uro-selective activity. (nih.gov)
  • A series of arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines was synthesized to develop new α 1 -adrenoceptor antagonists with uroselective profile. (nih.gov)
  • A series of trans-N-alkyl-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanemethylamines was synthesized and characterized for binding and function at the melanocortin-4 receptor (MC4R), and several potent benzylamine derivatives were identified. (nih.gov)
  • A QSAR Study of Matrix Metalloproteinases Type 2 (MMP-2) Inhibitors with Cinnamoyl Pyrrolidine Derivatives. (biomedsearch.com)
  • A multivariate PLS-QSAR study with a data set of 31 cinnamoyl pyrrolidine derivatives described as type 2 matrix metalloproteinases (MMP-2) inhibitors is presented in this paper. (biomedsearch.com)
  • Several 2-(aminomethyl)-and 2-(2-aminoethyl)-pyrrolidine-3,4-diol derivatives have been assayed for their inhibitory activities towards glycosidases. (epfl.ch)
  • The gold(I)-catalyzed reaction of methylenecyclopropanes with sulfonamides produces the corresponding pyrrolidine derivatives in moderate to good yields via a domino ring-opening ring-closing hydroamination process. (organic-chemistry.org)
  • Preparation of heteroaryl acyl pyrrolidine derivatives as antiviral agents. (qub.ac.uk)
  • The present invention relates to fungicidal 1-(heterocyclic carbonyl)-2-substituted pyrrolidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. (patentsencyclopedia.com)
  • The present invention relates to a new process for preparing 2-oxo-1-pyrrolidine derivatives of general formula (I), comprising the cyclisation of an intermediate of general formula (II) wherein the substituents are as defined in the specification. (expiredip.com)
  • Pyrrolidine dithiocarbamate (PDTC) is are a family of closely related drugs used for a metal chelation, induction of G1 phase cell cycle arrest, and preventing induction of nitric oxide synthase. (wikipedia.org)
  • Pyrrolidine dithiocarbamate binds zinc such that the resulting complex can enter the cell and inhibit viral RNA-dependent RNA polymerase. (wikipedia.org)
  • The aim of this study was to evaluate the effects of pyrrolidine dithiocarbamate on anxiety of streptozotocin-induced diabetic mouse using the open field and the elevated plus maze tests. (ijpsonline.com)
  • 16.7 mM/l of blood glucose) were treated with pyrrolidine dithiocarbamate or 0.9% saline for 10 w. (ijpsonline.com)
  • After pyrrolidine dithiocarbamate treatment, mice showed a higher % of time retention in open arms and higher percentage of entries in open arms than the diabetic group in the elevated plus maze. (ijpsonline.com)
  • In conclusion, pyrrolidine dithiocarbamate treatment in diabetic mice exerted anxiolytic-like effects. (ijpsonline.com)
  • Pyrrolidine dithiocarbamate (PDTC) is an antioxidant and is recently reported to inhibit ubiquitin-proteasome-mediated proteolysis. (asm.org)
  • Pyrrolidine dithiocarbamate (PDTC) antagonizes the cellular responsiveness to IL-6 through impairment in signal transducer and activator of transcription-3 activation and downstream signaling. (aspetjournals.org)
  • Relative contribution of NF-kappaB and AP-1 in the modulation by curcumin and pyrrolidine dithiocarbamate of the UVB-induced cytokine expression by keratinocytes. (inserm.fr)
  • To investigate in keratinocytes the relative contributions of those transcription factors on UVB-mediated cytokine induction, cell cultures were supplemented with curcumin and pyrrolidine dithiocarbamate (PDTC), agents known to modulate NF-kappaB and AP-1 activation. (inserm.fr)
  • In the current study, we investigate whether clioquinol (CQ), an analog of 8-hydroxyquinoline and an Alzheimer's disease drug, and pyrrolidine dithiocarbamate (PDTC), a known copper-binding compound and antioxidant, can interact with copper to form cancer-specific proteasome inhibitors and apoptosis inducers in human breast cancer cells. (biomedcentral.com)
  • The induction of this transcription factor can be blocked by a wide range of antioxidants, including pyrrolidine dithiocarbamate (PDTC). (elsevier.com)
  • Pyrrolidine dithiocarbamate attenuates t. (comu.edu.tr)
  • We aimed to demonstrate the potential protective effects of pyrrolidine dithiocarbamate (PDTC) on monocrotaline (MCT)-induced pulmonary arterial hypertension (PAH). (comu.edu.tr)
  • Pyrrolidine is used as a building block in the synthesis of more complex organic compounds. (wikipedia.org)
  • Sigma-Aldrich has a large selection of pyrrolidines as heterocyclic building blocks for organic synthesis and medicinal chemistry, the majority of which are available as racemates or in either enantiomeric form. (sigmaaldrich.com)
  • The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. (mdpi.com)
  • Pyrrolidine-2,5-dione derivates are an important class of heterocylic compounds with essential applications in medicinal chemistry and organic synthesis. (iucr.org)
  • Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 re. (nih.gov)
  • Palladium-catalyzed intramolecular amination of unactivated C-H bonds at the γ and δ positions of picolinamide (PA) protected amine substrates enables the synthesis of azetidine, pyrrolidine, and indoline compounds. (organic-chemistry.org)
  • For an upscale compatible multigram synthesis of the functionalized pyrrolidine scaffolds, we used a chiral pool synthetic route starting from methionine. (uni-koeln.de)
  • We describe here the synthesis of these compounds which are biaryl pyrrolidine and tetrahydrofuran sulfonamides and disclose their activities against the human GluA2 flip isoform homotetrameric receptor. (sussex.ac.uk)
  • Allylic Azide Rearrangement in Tandem with Intramolecular Huisgen Cycloaddition for Iminosugar and Glycomimetic Synthesis: Functionalized Piperidine, Pyrrolidine, and Pyrrolotriazoles from d-Mannose. (nuigalway.ie)
  • The present invention is directed to certain novel compounds identified as substituted piperidines, pyrrolidines and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R 1 , R 4 , R 5 , A, X, Y and n are as defined herein. (freepatentsonline.com)
  • Allylic azide rearrangement to secondary azides occurred in tandem with triazoline formation and this intermediate was then decomposed in the presence of nucleophilic reagents to give pyrrolidines, piperidines, or azepanes depending on whether cyclic constraint was incorporated or not, on diol stereochemistry and on the nucleophile. (nuigalway.ie)
  • These compounds are synthesized from b-aryl pyrrolidines, providing products with the 2-arylethyl amine moiety, a structural feature often encountered in compounds active in the central nervous system. (mdpi.com)
  • The title compound, 1'-(benzyloxy)-5'-cyanomethyl-2,3-dihydrospiro [inden-1,2'-pyrrolidine], ( trans-IIIa ), belongs to the family of spirocyclic compounds. (iucr.org)
  • Our data suggests chiral ribose-like pyrrolidine scaffolds have interesting potential for modifications of pharmacologically active compounds. (uni-koeln.de)
  • Chemical examination of the fungus Aspergillus ustus isolated from the Mediterranean sponge Suberites domuncula yielded the five new ophiobolin-type sesterterpenoids 1-5 and the two new pyrrolidine alkaloids 6 and 7, together with the known compound aurantiamine and cerebroside D. The structures of the new compounds were unambiguously elucidated on the basis of extensive spectroscopic-data analysis (1D- and 2D-NMR, MS, and UV) and comparison with literature data. (elsevier.com)
  • Pyrrolidine and piperidine are organic compounds that have cyclic structures. (differencebetween.com)
  • Compounds of formula I are novel with the exception of (RS)-2-phenyl-l~ (toluene-4-sulfonyl)-pyrrolidine, (RS)-l-(toluene-4-sulfonyl)-2-p-tolyl-pyrrolidine, N-tosyl-cis-3-methyl-2-phenyI pyrrolidine, 3-[ l-(toluene-4-sulfonyl)-pyrrolidin-2-yljpyridine and N-tosyl-2-(3,4-dimethoxy-phenyl)-pyrrolidine. (allindianpatents.com)
  • Chiral pyrrolidines play an important role both as chiral building blocks for auxiliaries as well as key structures relevant to biologically active substances. (sigmaaldrich.com)
  • A new chiral mesoporous hybrid material was synthesized based on pyrrolidine units included in a siliceous framework, HybPyr, and integrated into the organic-inorganic structure, from a specific bis-silylated precursor. (rsc.org)
  • Two dimeric chiral (pyrrolidine salen)Mn(III) complexes 3 and 4 were prepared, in which the two (pyrrolidine salen)Mn(III) units are linked either by a p-xylylene or by ap-phthalyl bridge. (diva-portal.org)
  • A series of chiral (pyrrolidine salen)Mn(III) complexes were synthesized front N-aza-substituted (R,R)-N,N'-bis(3,5-di-tert-butylsalicylidene)-3.4-diaminopyrrolidine salen ligands. (diva-portal.org)
  • In this study, we report on the modification of a 3,4-diaryl-isoxazole-based CK1 inhibitor with chiral pyrrolidine scaffolds to develop potent and selective CK1 inhibitors. (uni-koeln.de)
  • Rocha Gonsalves, " Chiral Pyrrolidine-Based Salen Ligands for the Enantioselective Alkylation of Aromatic Aldehydes", Letters in Organic Chemistry (2007) 4: 80. (eurekaselect.com)
  • By use of pyrrolidine as core structure, symmetric 3,4-bis-N-alkylsulfonamides were designed and synthesized enantioselectively from D-(-)-tartaric acid as a new class of HIV protease inhibitors. (rcsb.org)
  • We have developed a novel series of pyrrolidine derived BACE-1 inhibitors. (nih.gov)
  • 3R,4S)-4-(3-Bromophenyl)-1-(tert-butoxycarbonyl)-pyrrolidine-3-carboxylic Acid is used to prepare substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors, aryl substituted pyrrolidines. (trc-canada.com)
  • Relative to many secondary amines, pyrrolidine is distinctive because of its compactness, a consequence of its cyclic structure. (wikipedia.org)
  • Pyrrolidines are cyclic secondary amines with a five-membered ring, containing four carbon atoms and one nitrogen atom. (sigmaaldrich.com)
  • Maryam Hajjami, Arash Ghorbani-Choghamarani and Zahra Khani, "L-Pyrrolidine-2-Carboxylic Acid-4-Hydrogen Sulfate (Supported on Silica Gel) as a New and Efficient Catalyst for Acylation of Alcohols, Phenols and Amines Under Solvent-Free Conditions", Letters in Organic Chemistry (2013) 10: 324. (eurekaselect.com)
  • Interestingly, (2S,3R,4S)-2-{2-[(4-phenyl)phenylamino]ethyl}pyrrolidine-3,4-diol (12g) inhibits several enzymes, for instance alpha-L-fucosidase from bovine epididymis (K-i = 6.5 muM, competitive), alpha-galactosidase from bovine liver (K-i = 5 muM, mixed) and alpha-mannosidase from jack bean (K-i = 102 muM, mixed). (epfl.ch)
  • Diamines such as (2R,3S,4R)-2-[2-(phenylamino) or 2-(benzylamino)ethyl]pyrrolidine-3,4-diol (ent-1 2a, ent-12b) inhibit P-glucosidase from almonds (K-i = 13-40 muM, competitive). (epfl.ch)
  • The report provides key statistics on the market status of the S-(-)-1-Ethyl-2-Aminomethyl Pyrrolidine manufacturers and is a valuable source of guidance and direction for companies and individuals interested in the industry. (rnrmarketresearch.com)
  • An intermediate compound l-{2-[4-(6-Methoxy-3,4-dihydronaphthalen -l-yl)phenoxy] ethyl}pyrrolidine, or l-{2-[4-(2-Bromo-6-methoxy-3,4-dihydronaphthalen-l- yl)phenoxy]ethyl} pyrrolidine. (allindianpatents.com)
  • It captures n-methyl pyrrolidine market trends, pays close attention to n-methyl pyrrolidine manufacturers and names suppliers. (marketpublishers.com)
  • Find the (S)-1-(2-Chloroacetyl)pyrrolidine-2-carboxaMide 20605-41-8 products at Zaiqi Bio-Tech, one of the leading manufacturers and suppliers in this field. (pharmsynth.com)
  • Find the tert-butyl (S)-2-(2-hydroxyethyl)pyrrolidine-1-carboxylate 88790-38-9 products at Zaiqi Bio-Tech, one of the leading manufacturers and suppliers in this field. (pharmsynth.com)
  • Find the 2-(3-fluorophenyl)pyrrolidine 298690-72-9 products at Zaiqi Bio-Tech, one of the leading manufacturers and suppliers in this field. (pharmsynth.com)
  • Welcome to purchase the pyrrolidine products from Zaiqi Bio-Tech which is well-known as one of the leading manufacturers and suppliers in China. (pharmsynth.com)
  • In the title compound, C 13 H 15 NO 3 , the pyrrolidine ring makes a dihedral angle of 4.69 (9)° with the 3-meth-oxy-phenyl ring. (iucr.org)
  • R4 signifies, independently from each other, hydrogen or(C1-C7)-a1kyl, with the exception of (RS)-2-phenyl-l-( toluene-4-sulfonyl)-pyrrolidine, (RS)-l- (toluene-4-sulfo nyl) -2 -p- tolyl-pyrrolidine, N -tosyl-cis-3-methyl- 2-phenyl pyrrolidine, 3-[1-(toluene-4-sulfonyl)-pyrrolidin-2-yl]pyridine and N-tosyl-2-(3,4- dim ethoxy- phenyl) -pyrrolidin e, as well as their pharmaceutically acceptable salts. (allindianpatents.com)
  • Furthermore, the preparation of (RS)-2-phenyl-l-(toluene-4-sulfonyl)-pyrrolidine is described in Liebigs Ann. (allindianpatents.com)
  • Pyrrolidine, also known as tetrahydropyrrole, is an organic compound with the molecular formula (CH2)4NH. (wikipedia.org)
  • In the title compound, Fig. 1, the pyrrolidine ring (N1/C10-C13) makes a dihedral angle of 4.69 (9)° with the benzene ring (C2-C7). (iucr.org)
  • However, pyrrolidine is a naturally occurring compound we can find in different alkaloids such as nicotine. (differencebetween.com)
  • The key difference between pyrrolidine and piperidine is that pyrrolidine contains a five-membered ring, whereas piperidine contains a six-membered ring . (differencebetween.com)
  • The ''Global and Chinese (S)-(+)-2-(Methoxymethyl)pyrrolidine Industry, 2011-2021 Market Research Report'' is a professional and in-depth study on the current state of the global (S)-(+)-2-(Methoxymethyl)pyrrolidine industry with a focus on the Chinese market. (reportsnreports.com)
  • The report provides key statistics on the market status of the (S)-(+)-2-(Methoxymethyl)pyrrolidine manufacturers and is a valuable source of guidance and direction for companies and individuals interested in the industry.Firstly, the report provides a basic overview of the industry including its definition, applications and manufacturing technology. (reportsnreports.com)
  • Through the statistical analysis, the report depicts the global and Chinese total market of (S)-(+)-2-(Methoxymethyl)pyrrolidine industry including capacity, production, production value, cost/profit, supply/demand and Chinese import/export. (reportsnreports.com)
  • The report then estimates 2016-2021 market development trends of (S)-(+)-2-(Methoxymethyl)pyrrolidine industry. (reportsnreports.com)
  • In the end, the report makes some important proposals for a new project of (S)-(+)-2-(Methoxymethyl)pyrrolidine Industry before evaluating its feasibility. (reportsnreports.com)
  • Overall, the report provides an in-depth insight of 2011-2021 global and Chinese (S)-(+)-2-(Methoxymethyl)pyrrolidine industry covering all important parameters. (reportsnreports.com)
  • 5.2 Market Competition of (S)-(+)-2-(Methoxymethyl)pyrrolidine Industry by Country (USA, EU, Japan, Chinese etc. (reportsnreports.com)
  • 1-{3-[3-(methoxymethyl)pyrrolidine-1-carbonyl]benzenesulfonyl}-4-methyl-3,6-dih. (chembase.cn)
  • The b-aryl pyrrolidines are synthesized through a three-step methodology that includes a Knoevenagel condensation reaction, a 1,3-dipolar cycloaddition reaction, and a nitrile reduction. (mdpi.com)
  • Subsequent aza-Wacker oxidative cyclization or conjugate addition of the olefinated intermediates provides a variety of C-2 alkylated pyrrolidines. (scripps.edu)
  • The report includes n-methyl pyrrolidine description, covers its application areas, manufacturing methods, patents. (marketpublishers.com)
  • We provide independent and unbiased information on manufacturers, prices, production news and consumers for the global and regional (North America, Asia and Europe) market of pyrrolidine-1-carbonyl chloride. (reportsnreports.com)
  • Nitrogen-centered radical cyclizations onto silyl enol ethers were utilized for the syntheses of protected polyhydroxylated pyrrolidines 2-hydroxymethyl-3-hydroxypyrrolidine and 1,4-dideoxy-1,4-imino-L-ribitol. (ubc.ca)
  • N-Methyl Pyrrolidine (CAS 120-94-5) Market Research Report 2019 aims at providing comprehensive data on n-methyl pyrrolidine market globally and regionally (Europe, Asia, North America, Latin America etc. (marketpublishers.com)
  • The alkenes' access pathway is discussed on the basis of the steric effect of the N-aza-substituent in the pyrrolidine backbone of complexes 1-3 on the enantioselectivity of epoxidation. (diva-portal.org)
  • Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgetics. (epo.org)
  • EP0542136A1 ] Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. (epo.org)
  • The pyrrolidine ring structure is present in numerous natural alkaloids such as nicotine and hygrine. (wikipedia.org)
  • Using AlCl 3 as the catalyst, pyrrolidones were solely obtained at room temperature, while RuCl 3 as the catalyst selectively afforded pyrrolidines in high yields at 45 °C. (rsc.org)
  • Pyrrolidine is prepared industrially by the reaction of 1,4-butanediol and ammonia at a temperature of 165-200 °C and a pressure of 17-21 MPa in the presence of a cobalt- and nickel oxide catalyst, which is supported on alumina. (wikipedia.org)
  • RTI-229 , also known as (-)-3β-(4-iodophenyl)tropane-2β-pyrrolidine carboxamide and RTI- 4229 -229 , is a potent and long-lasting stimulant drug which was developed in the 1990s as part of a large group of related analogues from the phenyltropane family. (wikipedia.org)
  • In the laboratory, pyrrolidine was usually synthesised by treating 4-chlorobutan-1-amine with a strong base: Many modifications of pyrrolidine are found in natural and synthetic chemistry. (wikipedia.org)
  • piperidine, pyrrolidine, and perhydroazepine to provide $\alpha$-lithioamine synthetic equivalents. (illinois.edu)