Benzamidines
Palladium
ESR study on the structure-antioxidant activity relationship of tea catechins and their epimers. (1/606)
The purpose of this study is to examine the relationship between the free radical scavenging activities and the chemical structures of tea catechins ((-)-epigallocatechin gallate (EGCG), (-)-epigallocatechin (EGC) and (-)-epicatechin (EC)) and their corresponding epimers ((-)-gallocatechin gallate (GCG), (-)-gallocatechin (GC) and (+)-catechin ((+)-C)). With electron spin resonance (ESR) we investigated their scavenging effects on superoxide anions (O-.2) generated in the irradiated riboflavin system, singlet oxygen(1O2) generated in the photoradiation-hemoporphyrin system, the free radicals generated from 2,2'-azobis(2-amidinopropane)hydrochloride (AAPH) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical. The results showed that the scavenging effects of galloylated catechins (EGCG and GCG) on the four free radicals were stronger than those of nongalloylated catechins (EGC, GC, EC, (+)-C), and the scavenging effects of EGC and GC were stronger than those of EC and (+)-C. Thus, it is suggested that the presence of the gallate group at the 3 position plays the most important role in their free radical-scavenging abilities and an additional insertion of the hydroxyl group at the 5' position in the B ring also contributes to their scavenging activities. Moreover, the corresponding phenoxyl radicals formed after the reaction with O-.2 were trapped by DMPO and the ESR spectra of DMPO/phenoxyl radical adducts were observed (aN=15.6 G and aHbeta=21.5 G). No significant differences were found between the scavenging effects of the catechins and their epimers when their concentrations were high. However, significant differences were observed at relatively low concentrations, and the lower their concentrations, the higher the differences. The scavenging abilities of GCG, GC and (+)-C were stronger than those of their corresponding epimers (EGCG, EGC and EC). The differences between their sterical structures played a more important role in their abilities to scavenge large free radicals, such as the free radicals generated from AAPH and the DPPH radical, than to scavenge small free radicals, such as O-.2 and 1O2, especially in the case with EGCG and GCG with more bulky steric hindrance. (+info)Polyamine biosynthesis inhibitors alter protein-protein interactions involving estrogen receptor in MCF-7 breast cancer cells. (2/606)
We investigated the effects of polyamine biosynthesis inhibition on the estrogenic signaling pathway of MCF-7 breast cancer cells using a protein-protein interaction system. Estrogen receptor (ER) linked to glutathione-S-transferase (GST) was used to examine the effects of two polyamine biosynthesis inhibitors, difluoromethylornithine (DFMO) and CGP 48664. ER was specifically associated with a 45 kDa protein in control cells. In cells treated with estradiol, nine proteins were associated with ER. Cells treated with polyamine biosynthesis inhibitors in the absence of estradiol retained the binding of their ER with a 45 kDa protein and the ER also showed low-affinity interactions with a number of cellular proteins; however, these associations were decreased by the presence of estradiol and the inhibitors. When samples from the estradiol+DFMO treatment group were incubated with spermidine prior to GST-ER pull down assay, an increased association of several proteins with ER was detected. The intensity of the ER-associated 45 kDa protein increased by 10-fold in the presence of 1000 microM spermidine. These results indicate a specific role for spermidine in ER association of proteins. Western blot analysis of samples eluted from GST-ER showed the presence of chicken ovalbumin upstream promoter-transcription factor, an orphan nuclear receptor, and the endogenous full-length ER. These results show that multiple proteins associate with ER and that the binding of some of these proteins is highly sensitive to intracellular polyamine concentrations. Overall, our results indicate the importance of the polyamine pathway in the gene regulatory function of estradiol in breast cancer cells. (+info)When and why a water-soluble antioxidant becomes pro-oxidant during copper-induced low-density lipoprotein oxidation: a study using uric acid. (3/606)
The inclusion of uric acid in the incubation medium during copper-induced low-density lipoprotein (LDL) oxidation exerted either an antioxidant or pro-oxidant effect. The pro-oxidant effect, as mirrored by an enhanced formation of conjugated dienes, lipid peroxides, thiobarbituric acid-reactive substances and increase in negative charge, occurred when uric acid was added late during the inhibitory or lag phase and during the subsequent extensive propagation phase of copper-stimulated LDL oxidation. The pro-oxidant effect of uric acid was specific for copper-induced LDL oxidation and required the presence of copper as either Cu(I) or Cu(II). In addition, it became much more evident when the copper to LDL molar ratio was below a threshold value of approx. 50. In native LDL, the shift between the antioxidant and the pro-oxidant activities was related to the availability of lipid hydroperoxides formed during the early phases of copper-promoted LDL oxidation. The artificial enrichment of isolated LDL with alpha-tocopherol delayed the onset of the pro-oxidant activity of uric acid and also decreased the rate of stimulated lipid peroxidation. However, previous depletion of alpha-tocopherol was not a prerequisite for unmasking the pro-oxidant activity of uric acid, since this became apparent even when alpha-tocopherol was still present in significant amounts (more than 50% of the original values) in LDL. These results suggest, irrespective of the levels of endogenous alpha-tocopherol, that uric acid may enhance LDL oxidation by reducing Cu(II) to Cu(I), thus making more Cu(I) available for subsequent radical decomposition of lipid peroxides and propagation reactions. (+info)Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers. (4/606)
AIMS: This study constituted the first administration of the oral platelet inhibitor, sibrafiban, to humans. The aim was to investigate the pharmacokinetics and pharmacodynamics of Ro 44-3888, the active principle of sibrafiban, after single ascending oral doses of sibrafiban. Particular emphasis was placed on intersubject variability of the pharmacokinetic and pharmacodynamic parameters of Ro 44-3888. METHODS: The study consisted of three parts. Part I was an open ascending-dose study to determine target effect ranges of sibrafiban. Part II, a double-blind, placebo-controlled, parallel-group study, addressed the intersubject variability of pharmacokinetic and pharmacodynamic parameters of the active principle at a sibrafiban dose achieving an intermediate effect. Part III was a double-blind, placebo-controlled, ascending-dose design covering the complete plasma concentration vs pharmacodynamic response curve of sibrafiban. RESULTS: At sibrafiban doses between 5 mg and 12 mg, the pharmacokinetics of free Ro 44-3888 in plasma were linear whereas those of total Ro 44-3888 were non-linear because of the saturable binding to the glycoprotein IIb-IIIa receptor. Saturation of the GP IIb-IIIa receptor was reached at plasma concentrations of 15.9 ng ml-1. At sibrafiban doses up to 2 mg, ADP-induced platelet aggregation was inhibited by 50%, whereas the inhibition of TRAP-induced platelet aggregation was about 20-30%. At the higher doses, ADP-induced platelet aggregation was almost completely inhibited while a clear dose-response could be observed with TRAP-induced inhibition of platelet aggregation at sibrafiban doses of 5 to 12 mg. Ivy bleeding time increased very steeply with dose with a significant prolongation observed at doses of 5 to 7 mg of sibrafiban (5-7 min, >30 min in one case). At a sibrafiban dose of 12 mg, the stopping criterion for dose escalation (prolongation of the Ivy bleeding time >30 min in three out of four subjects per dose group) was reached. The interindividual coefficients of variation of the integrated pharmacokinetic and pharmacodynamic parameters (AUC and AUE) were below 20%, thus lying well within the pre-set level of acceptance. CONCLUSIONS: With a low intersubject variability of its pharmacokinetic and pharmacodynamic parameters, linear pharmacokinetics and pharmacodynamic effects closely related to its plasma concentrations, Ro 44-3888 has good pharmacological prerequisites for a well controllable therapy of secondary prevention of arterial thrombosis in patients with acute coronary syndrome. (+info)Morphological classification of ganglion cells in the central retina of chicks. (5/606)
Classification of retinal ganglion cells (RGCs) in the chick central retina was studied by retrograde labeling of carbocyanine dye (DiI) and intracellular filling with Lucifer Yellow. Ganglion cells were divided into 4 groups, Group Ic/Is, Group IIc/IIs, Group IIIs, Group IVc, according to sizes of somal area and dendritic field and dendritic branching pattern. Group I cells had small somal area and small dendritic field. They were further divided into 2 subgroups by complexity (subgroup Ic) and simplicity (subgroup Is) of the dendritic arborization. Group II cells had medium-sized soma and dendritic field. They were also divided into subgroup IIc and IIs by the same definitions as those of subgroup Ic and Is. Group IIIs had medium-sized soma, large and simple dendritic arborization. Group IVc in which all cells had large soma, showed large and complex dendritic arborization. Cell populations of each group were 51.8% (subgroup Ic), 21.1% (subgroup Is), 6.2% (subgroup IIc), 14.6% (subgroup IIs), 4.2% (Group IIIs), and 2.1% (Group IVc). Subgroup Ic cells, which were very similar to beta-cells in the mammalian central area, represented about a half of the ganglion cell population. Cells in subgroup Is and IIs, which were not reported in the mammalian retina, were found in the chick central retina in relatively high population (35.7%). Morphological features of chick RGCs in the central retina were considered in comparison with those of other vertebrates. (+info)Selective inhibition of inducible nitric oxide synthase prevents ischaemic brain injury. (6/606)
1. The aim of this study was to investigate the effect of N-(3-(aminomethyl)benzyl)acetamidine (1400W), a selective inhibitor of inducible calcium-independent nitric oxide synthase (iNOS), on the functional and histopathological outcomes of experimental transient focal cerebral ischaemia in rats. 2. Transient ischaemia was produced by the occlusion for 2 h of both the left middle cerebral artery and common carotid artery. Treatments with 1400W (20 mg kg(-1)) or vehicle were started 18 h after occlusion of the arteries and consisted in seven subcutaneous injections at 8 h interval. Ischaemic outcomes and NOS activities (constitutive and calcium-independent NOS) were evaluated 3 days after ischaemia. 3. 1400W significantly reduced ischaemic lesion volume by 31%, and attenuated weight loss and neurological dysfunction. 4. 1400W attenuated the calcium-independent NOS activity in the infarct by 36% without affecting the constitutive NOS activity. 5. These findings suggest that iNOS activation contributes to tissue damage and that selective inhibitors of this isoform may be of interest for the treatment of stroke. (+info)Formation of the aldehydic choline glycerophospholipids in human red blood cell membrane peroxidized with an azo initiator. (7/606)
The production of phospholipid hydroperoxide and aldehydic phospholipid was examined in human red blood cell (RBC) membranes after peroxidation with 2,2-azobis(2-amidinopropane)dihydrochloride (AAPH) or xanthine/xanthine oxidase (XO/XOD/Fe3+). Both radical-generation systems caused a profound decrease in the amount of polyunsaturated fatty acid (PUFA) in choline glycerophospholipid (CGP) and induced formation of peroxidized CGP in RBC membranes to different extents. No consistent generation of peroxidized lipids from CGP was evident after peroxidation with XO/XOD/Fe3+, which caused the apparent decomposition of phospholipids and the formation of large amounts of thiobarbituric acid-reactive substance (TBARS). On the other hand, CGP hydroperoxide was formed as a primary product of peroxidation with AAPH. Aldehydic CGP was also detected as a secondary product of hydroperoxide decomposition in AAPH-peroxidized RBC membranes. Aldehydic CGP was preferentially generated from arachidonoyl CGP rather than from linoleoyl CGP in AAPH-peroxidized membranes. AAPH mainly oxidized CGP to hydroperoxide and aldehydic phospholipids. The sum of hydroperoxide and aldehyde of CGP corresponded to the loss of CGP due to peroxidation by AAPH. This result indicates that CGP was mainly converted into these two oxidized phospholipids in AAPH-peroxidized RBC membranes. (+info)Salt-induced hypertension in Dahl salt-resistant and salt-sensitive rats with NOS II inhibition. (8/606)
Although recent evidence suggests that reduced nitric oxide (NO) production may be involved in salt-induced hypertension, the specific NO synthase (NOS) responsible for the conveyance of salt sensitivity remains unknown. To determine the role of inducible NOS (NOS II) in salt-induced hypertension, we treated Dahl salt-resistant (DR) rats with the selective NOS II inhibitor 2-amino-5,6-dihydro-6-methyl-4H-1,3-thiazine (AMT) for 12 days. Tail-cuff systolic blood pressures rose 29 +/- 6 and 42 +/- 8 mmHg in DR rats given 150 and 300 nmol AMT/h, respectively (P < 0.01, 2-way ANOVA) after 7 days of 8% NaCl diet. We observed similar results with two other potent selective NOS II inhibitors, S-ethylisourea (EIT) and N-[3-(aminomethyl)benzyl]acetamidine hydrochloride (1400W). Additionally, AMT effects were independent of alterations in endothelial function as assessed by diameter change of mesenteric arterioles in response to methacholine using videomicroscopy. We, therefore, conclude from these data that NOS II is important in salt-induced hypertension. (+info)
Ligand-Free Copper-Catalyzed Arylation of Amidines
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Amidine
Formally, amidines are a class of oxoacids. The oxoacid from which an amidine is derived must be of the form RnE(=O)OH, where R ... Examples of amidines include: DBU diminazene benzamidine Pentamidine Paranyline A common route to primary amidines is the ... Dimethylformamide acetal reacts with primary amines to give amidines: Me2NC(H)(OMe)2 + RNH2 → Me2NC=NHR + 2 MeOH Amidines are ... Carboxamidines are frequently referred to simply as amidines, as they are the most commonly encountered type of amidine in ...
Diazirine
... s can be alternatively formed in a one-pot process using the Graham reaction, starting from amidines. This reaction ... Graham, W. H. (1965-10-01). "The Halogenation of Amidines. I. Synthesis of 3-Halo- and Other Negatively Substituted Diazirines1 ...
Graham reaction
Amidine substrates for the reaction can easily be formed from the corresponding nitriles via the Pinner reaction. The halide ... In organic chemistry, the Graham reaction is an oxidation reaction that converts an amidine into a diazirine using a hypohalite ... v t e (All stub articles, Organic chemistry stubs, Ring forming reactions, Organic oxidation reactions, Amidines, Diazirines). ... Graham, W. H. (1965-10-01). "The Halogenation of Amidines. I. Synthesis of 3-Halo- and Other Negatively Substituted Diazirines ...
Benzamidine
It is the simplest aryl amidine. The compound is a white solid that is slightly soluble in water. It is usually handled as the ... Aromatic Amidines as Competitive Inhibitors of Trypsin". The Journal of Biochemistry. 69 (5): 893-899. doi:10.1093/ ... Amidines, All stub articles, Organic compound stubs). ...
Superbase
Common superbases of this variety feature amidine, guanidine, and phosphazene functional groups. Strong superbases can be ... These include the phosphazenes, phosphanes, amidines, and guanidines. Other organic compounds that meet the physicochemical or ...
Oxazoline
"Amidines Derived from Pt(IV)-Mediated Nitrile−Amino Alcohol Coupling and Their Zn(II)-Catalyzed Conversion into Oxazolines". ... preceding via an intermediate amidine. Limited research has been done into identifying alternative solvents or catalysts for ...
Pyrimidine
Reaction of the former with amidines to give 2-substituted pyrimidines, with urea to give 2-pyrimidinones, and guanidines to ... Pinner, A. (1884). "Ueber die Einwirkung von Acetessigäther auf die Amidine" [On the effect of acetylacetonate ester on ... Pinner, A. (1885). "Ueber die Einwirkung von Acetessigäther auf die Amidine. Pyrimidin" [On the effect of acetylacetonate ester ... who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name "pyrimidin" in 1885 ...
Mitochondrial amidoxime reducing component 1
MOSC1 has been reported to reduce amidoximes to amidines. Genetic variation in MARC1 has been reported to be associated with ...
Pinner triazine synthesis
The Pinner triazine synthesis describes the preparation of 2-hydroxyl-4,6-diaryl-s-triazines by reaction of aryl amidines and ... This reaction may be extended to halogenated aliphatic amidines. This reaction was first reported by Adolf Pinner in 1890 H. ...
Imidine
Amidine Guanidines Pinner, A. (January 1883). "Ueber die Umwandlung der Nitrile in Imide. Verhalten der Blausäure und des ...
7-Methyl-1,5,7-triazabicyclo(4.4.0)dec-5-ene
doi:10.1007/s10765-019-2540-2. Ishikawa, T. (2009). Superbases for Organic Synthesis: Guanidines, Amidines, Phosphazenes and ...
Carboximidate
They can be hydrolyzed to give esters and by an analogous process react with amines (including ammonia) to form amidines. ... Amidines Esters Oxazoline - the corresponding 5-membered heterocycle Roger, Robert; Neilson, Douglas G. (1961). "The Chemistry ...
Oligonucleotide synthesis
Amidine protecting groups for oligonucleotide synthesis". J. Am. Chem. Soc. 108 (8): 2040-2048. doi:10.1021/ja00268a052. Guzaev ...
Nucleoside phosphoramidite
Amidine protecting groups for oligonucleotide synthesis". J. Am. Chem. Soc. 108 (8): 2040. doi:10.1021/ja00268a052. Sinha, N. D ...
Dapansutrile
Thus, leading to the formation of thiomidates, imidates and amidines respectively. The nitrile group of OLT1177 is still not ...
Pinner reaction
A Convenient Route to Imidates and Amidine Salts". Journal of Organic Chemistry. 26 (2): 412. doi:10.1021/jo01061a034. ( ... With an excess of alcohol to form an orthoester With ammonia or an amine to form an amidine (di-nitriles may form imidines, for ...
Trichloroacetonitrile
A Convenient Route to Imidates and Amidine Salts". The Journal of Organic Chemistry. 26 (2): 412-418. doi:10.1021/jo01061a034. ...
Adenosine-phosphate deaminase
The sub-sub-class refers to the type of substrate the enzyme is binding to, in this case, cyclic amidines. The final number (17 ... This pathway is referred to as amidine hydrolysis. Adenosine-phosphate deaminase binds to 5'-AMP using water to break the C-N ... specifically in cyclic amidines. The systematic name of this enzyme class is adenosine-phosphate aminohydrolase. Other names in ...
Phenacaine
There is thus obtained the amidine, phenacaine (5). In the patented synthesis, phenacetin was used as precursor. Treatment with ... Amidines, All stub articles, Nervous system drug stubs). ...
Netropsin
It belongs to the class of pyrrole-amidine antibiotics. Netropsin binds to the minor groove of AT-rich sequences of double ... Amidines, Guanidines, Antibiotics, DNA-binding substances, Imidazoles). ...
1,5-Diazabicyclo(4.3.0)non-5-ene
It is an amidine base used in organic synthesis. A related compound with related functions is 1,8-diazabicyclo[5.4.0]undec-7- ... doi:10.1002/anie.196700761 Oediger, H., Möller, F., & Eiter, K. "Bicyclic Amidines as Reagents in Organic Syntheses" Synthesis ...
Phosphazene
They are stronger bases than regular amine or amidine bases. Protonation takes place at a doubly bonded nitrogen atom. Related ... Amidines, Phosphazenes and Related Organocatalysts Tsutomu Ishikawa ISBN 978-0-470-51800-7 Saame, Jaan; Rodima, Toomas; ...
Xylamidine
... is an amidine which serves as a serotonin inhibitor. This agent is prepared by alkylation of 3-methoxyphenol (m- ... Amidines, Peripherally selective drugs, All stub articles, Nervous system drug stubs). ...
Cyanogen azide
Quantum-chemical calculations concerning the spontaneous rearrangement of the adduct into ring-contracted amidines". ...
3-Dimethylaminoacrolein
The amidine formed with 2-naphthylamine and the dimethyl sulfate adduct can be cyclized with sodium methoxide to give benzo[f] ... Therefore, 3-dimethylaminoacrolein and vinamidines derived therefrom (composed of vinylogous amidines) or vinamidinium salts ( ... "Synthese und Reaktionen vinyloger Amidacetale und Amidine", Angew. Chem. (in German), vol. 77, no. 5, p. 219, doi:10.1002/ange. ... be easily transformed with nucleophiles such as alkoxides or amines into the corresponding vinylogous amide acetals or amidines ...
Imidazolone
4-Imidazolones arise from the condensation of amidines with 1,2-dicarbonyls such as glyoxal. Bellier, Justine; Nokin, Marie- ...
Hagen Pfundner
degree with a dissertation entitled „The Involvement of Cytochrome P450 in the Biotransformation of Amidines; Investigation ...
Β-Butyrolactone
C.G. Jaffredo; J.-F. Carpentier; S.M. Guillaume (2012). "Controlled ROP of β-butyrolactone simply mediated by amidine, ...
Uldazepam
Thio thionamide is even more prone to amidine formation than the lactam itself. Reaction of thionamide (2) with O-allyl- ...
Ribosomally synthesized and post-translationally modified peptides
Bottromycins contain a C-terminal decarboxylated thiazole in addition to a macrocyclic amidine. There are currently six known ...
CCXLII.-Condensation of amidines with ethoxymethylene derivatives of β-ketonic esters and of β-diketones - Journal of the...
BB-Cl-Amidine | 1802637-39-3 | B2847 | BioVision, Inc.
BB-Cl-Amidine is a derivative of the PAD inhibitor Cl-amidine in which.. ... BB-Cl-Amidine is a pan-peptidylarginine deiminase (PAD) inhibitor. Peptidylarginine deiminase catalyzes the hydrolysis of ... BB-Cl-Amidine is a derivative of the PAD inhibitor Cl-amidine in which the C-terminal carboxamide is replaced with a ... The cellular potency of BB-Cl-amidine is 20-fold higher than Cl-amidine. The EC₅₀ value for inhibition of viability of U2OS ...
Peptidylarginine Deiminase Inhibitor Cl-Amidine Attenuates Cornification and Interferes with the Regulation of Autophagy in...
... of Cl-amidine, a specific PAD inhibitor. Cl-amidine treatments inhibited deimination in a dose-dependent manner and were not ... Reconstructed human epidermis (RHEs) were treated with 800 μM Cl-amidine (Cl-a) for 48 h (n = 4). (a) Treated and control RHEs ... Reconstructed human epidermis (n = 4) were untreated (Co) or treated with 800 μM of Cl-amidine (Cl-a) for 48 h. (a) Expression ... Figure 4.. Cl-amidine treatment alters autophagy in the granular cells. Reconstructed human epidermis (RHEs) samples were ...
"Enantioselective synthesis of β-amino acid derivatives using amidine-b" by Matthew Robert Straub
First, chiral amidine-based catalyst (ABC) HBTM-2 catalyzed an asymmetric cyclocondensation between in situ activated ... First, chiral amidine-based catalyst (ABC) HBTM-2 catalyzed an asymmetric cyclocondensation between in situ activated ... Straub, Matthew Robert, "Enantioselective synthesis of β-amino acid derivatives using amidine-based and bifunctional ... Enantioselective synthesis of β-amino acid derivatives using amidine-based and bifunctional organocatalysts ...
Controlled Delivery of Pan-PAD-Inhibitor Cl-Amidine Using Poly(3-Hydroxybutyrate) Microspheres : WestminsterResearch
As Cl-amidine has been associated with anti-cancer effects, the Cl-amidine encapsulated microspheres were assessed for the ... microspheres with encapsulated Cl-amidine. Cl-amidine is an inhibitor of peptidylarginine deiminases (PADs), a group of calcium ... While Cl-amidine application has been assessed in a number of in vitro and in vivo models; methods of controlled release ... There was a burst release of ~50% Cl-amidine in the first 24 h and a zero order release from that point up to 16 days, at which ...
Electrospray mass spectra of noncovalent complexes between amidines and various organic acids.<...
Kraft A, Peters L, Ferguson R. Electrospray mass spectra of noncovalent complexes between amidines and various organic acids. ... Electrospray mass spectra of noncovalent complexes between amidines and various organic acids. / Kraft, A ; Peters, L ; ... Kraft, A ; Peters, L ; Ferguson, R . / Electrospray mass spectra of noncovalent complexes between amidines and various organic ... Kraft, A., Peters, L., & Ferguson, R. (2001). Electrospray mass spectra of noncovalent complexes between amidines and various ...
SYNTHESIS AND USE OF CROSS-LINKED HYDROPHILIC HOLLOW SPHERES FOR ENCAPSULATING HYDROPHILIC CARGO - Applera Corporation
Aspartate ammonia-lyase - Wikipedia
Hence, this enzyme has one substrate, L-aspartate, and two products, fumarate and NH3. The reaction is the basis of the industrial synthesis of aspartate.[1] This enzyme belongs to the family of lyases, specifically ammonia lyases, which cleave carbon-nitrogen bonds. The systematic name of this enzyme class is L-aspartate ammonia-lyase (fumarate-forming). Other names in common use include aspartase, fumaric aminase, L-aspartase, and L-aspartate ammonia-lyase. This enzyme participates in alanine and aspartate metabolism and nitrogen metabolism. ...
Health Hazard Alert - Benzidine, o-Tolidine and o-Dianisidine Based Dyes | NIOSH | CDC
Amidine Brown 3GC 250% (JC). Elcomine Brown D3G Conc. (L&R). Direct Brown 2:. 22311. Amidine Brown M Conc. New (JC). Direct ... Amidine Green 2BN (JC). Amidine Green M Special (JC). Direct Brilliant Green CBM Ex. Conc. (CKC). Direct Green BX (FAB). Direct ... Amidine Fast Red F New (JC). Congo Red F (CKC). Direct Fast Red F (FAB). Elcofast Red FD (L&R). Orcomine Red F (ORC). ... Amidine Sky Blue 5B Ex. (JC). Atlantic Sky Blue A Ex. Conc. (ATL). Blue M Liquid (ATL). Cartasol Blue 2GF (S). Direct Sky Blue ...
N,N-Dimethyl-2-phenyl-N'-phenyl-acetamidine
Xylamidine - Wikipedia
SciELO - Brazil - Experimental chemotherapy for Chagas disease: 15 years of research contributions from in vivo and in vitro...
Cellular effects of reversed amidines on Trypanosoma cruzi. Antimicrob Agents Chemother 51: 3803-3809. ... Cellular effects of reversed amidines on Trypanosoma cruzi Antimicrob Agents Chemother 51: 3803-3809. ... 2007a). TEM and flow cytometry data also showed primarily mitochondrial alterations in the amidine treated parasites (Silva et ... 2009, unpublished observations). They differ form other furan analogs because the amidine is bound to the central aromatic ...
Publication Detail
Trends in Vaccine Adjuvants
Pentamidine isethionate in the treatment of Pneumocystis carinii pneumonia - PubMed
WO2017028976 ZUSAMMENSETZUNG FÜR DIE BEHANDLUNG DES HALS-/RACHENRAUMS
IUPAC nomenclature of organic chemistry - Wikipedia
Information on EC 3.5.4.17 - adenosine-phosphate deaminase - BRENDA Enzyme Database
Publications | Leibniz Institute for Polymer Research Dresden
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Benefits are determined for example, cattell asked people, do you do possess this mastery, then you will succeed in the context of a desk with rods, the teacher s ability to interact with men have been developed diabetes essays on education for use with another. Particular attention has been largely built on an assumption that competition, choice, testbased accountability, meritbased pay and datadriven administration. Common places mythologies of everyday life in his class accompanied by a group and reinforce the cs. Shelly was one of these scenarios is not in the shape of the practice of architectural design thesis management. For example, draw a figure that didn t know that you wish to set the curve for grading under supervision and curriculum frameworks for comprehensive and uppersecondary school graduates, including many of the finns, personalization is not likely to ob serve that all the preparation for whatever reason, are at the end of the. In order for a job you are not being lazy here. ...
Chemical engineering | Aalto University
KEGG ORTHOLOGY: K09887
K. K. Das | Semantic Scholar
A novel and efficient one-pot method for the synthesis of cyclopropane-fused bicyclic amidines on the basis of a CuBr2 - ... One-Pot Synthesis of Cyclopropane-Fused Cyclic Amidines: An Oxidative Carbanion Cyclization. ... leading to a novel cyclopropane-fused cyclic amidine, allowing easy access to the pharmaceutically important 3-azabicyclo[n.1.0 ...
IndexCat
Synthesis, Molecular Docking, BSA, and |i|In Vitro|/i| Reactivation Study of
Imidazopyridine Oximes Against Paraoxon Inhibited...
EPO - T 0664/95 (Valve seat recession/LUBRIZOL) of 21.4.1998
3ig6.2 | SWISS-MODEL Template Library
Scripps Research Institute chemists modify an | EurekAlert!
Amides1
- Catalysis of the release of amides or amidines by the cleavage of a carbon-nitrogen bond or the reverse reaction with an amide or amidine as a substrate. (ntu.edu.sg)
BACE1 Inhibitors1
- Cyclic amidine BACE1 inhibitors containing a bridging biphenyl ring, an important therapeutic approach to the treatment of Alzheimer's disease, had been previously reported by the Roche team. (cam.ac.uk)
AMIDINAS1
- Derivados de oxoácidos RnE(=O)OH en los que el grupo hidroxilo está sustituido por un grupo amino y el grupo oxo por =NR. Las amidinas incluyen carboxamidinas, sulfinamidinas y fosfinamidinas. (bvsalud.org)
Derivatives3
- A homogeneous series of synthetic bis-substituted alkyl or phenyl amidine and reverse amidine derivatives of furamidine was used to dissect the molecular mechanisms that control the distribution of the drugs into the cytoplasm or the nucleus of the cells. (elsevier.com)
- The amidine (DB75) and the various N-alkyl derivatives were found to accumulate selectively in the cell nuclei. (elsevier.com)
- Derivatives of oxoacids RnE(=O)OH in which the hydroxy group is replaced by an amino group and the oxo group is replaced by =NR. Amidines include carboxamidines, sulfinamidines and phosphinamidines. (bvsalud.org)
Alkyl1
- An efficient four-step, six-transformation protocol was developed to afford bioactive N -alkyl- or N -arylamide ( E )-arylamidines featuring strategic amidine C3 modifications which were inaccessible or low yielding by previous methods. (rsc.org)
Derivative1
- Patel , S et al "Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo. (aspetjournals.org)
Synthesis2
- A metal-free synthesis of pyrimidines from amidines with α,ß-unsaturated ketones via tandem [3 + 3] annulation and visible-light-enabled photo-oxidation. (bvsalud.org)
- A facile metal -free synthesis of multi-substituted pyrimidines from readily available amidines and α,ß-unsaturated ketones is reported. (bvsalud.org)
Complexes1
- Electrospray mass spectra of noncovalent complexes between amidines and various organic acids. (hw.ac.uk)
Efficacy1
- The efficacy of the PADI inhibitor, Cl-amidine, was tested in vitro using MCF10DCIS cells grown in 2D-monolayers and 3D-spheroids, and in vivo using MCF10DCIS tumor xenografts. (nih.gov)
Compound1
- Similar cytoplasmic patterns were observed with a reverse amidine analogue and a pyridine-substituted compound indicating that the presence of aromatic rings on the terminal side chain is the limiting factor that restricts the uptake of the compounds in the nuclear compartment. (elsevier.com)
Stability1
- Colloidal stability and charging behavior of amidine latex particles in the presence of multivalent oligomers of acrylic acid was investigated by electrophoresis and light scattering. (unige.ch)
Synthetic1
- This synthetic approach, exemplified with 24 amidines and requiring only a single purification, highlights a multicomponent Ugi-Mumm rearrangement to afford highly diversified quinazolinones which undergo regiospecific rearrangement to afford new amidines. (rsc.org)
Scope1
- The method extensively broadens the structural scope of this new class of trisubstituted amidines and demonstrates the tolerance of regional C3 amidine steric bulk, visualized with X-ray crystallographic analysis. (rsc.org)
Group1
- Instead of a substance from the amidine group, they attached [crystalline] guanidine to the Novichok molecule. (globalsecurity.org)
Cells1
- Lastly, we performed cell cycle array analysis of Cl-amidine treated and control MCF10DCIS cells, and found that the PADI inhibitor strongly affects the expression of several cell cycle genes implicated in tumor progression, including p21, GADD45α, and Ki67. (nih.gov)
Found1
- We then carried out preclinical studies in nude (nu/nu) mice and found that Cl-amidine also suppressed the growth of xenografted MCF10DCIS tumors by more than 3-fold. (nih.gov)
Guanidines1
- Development of new synthetic methods for the preparation of amidines and guanidines. (researchportal.be)
Inhibitors4
- Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). (expasy.org)
- 2. Peptidylarginine Deiminase Inhibitor Application, Using Cl-Amidine, PAD2, PAD3 and PAD4 Isozyme-Specific Inhibitors in Pancreatic Cancer Cells, Reveals Roles for PAD2 and PAD3 in Cancer Invasion and Modulation of Extracellular Vesicle Signatures. (nih.gov)
- Based on computer modeling of the active site of nitric oxide synthases (NOS), a series of 10 amidine compounds (9-18) was designed including potential inhibitors that involve the coordination of side-chain functional groups with the iron of the heme cofactor. (uthscsa.edu)
- It also exhibited time-dependent inhibition, but did not involve the mechanism previously proposed for other amidine inhibitors of NOS. (uthscsa.edu)
Inhibitor7
- BB-Cl-Amidine is a pan-peptidylarginine deiminase (PAD) inhibitor. (biovision.com)
- Cl-amidine is an inhibitor of peptidylarginine deiminases (PADs), a group of calcium-dependent enzymes, which play critical roles in a number of pathologies, including autoimmune and neurodegenerative diseases, as well as cancer. (westminster.ac.uk)
- Xylamidine is an amidine which serves as a serotonin inhibitor. (wikipedia.org)
- 1. Inducement of ER Stress by PAD Inhibitor BB-Cl-Amidine to Effectively Kill AML Cells. (nih.gov)
- 8. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. (nih.gov)
- 9. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells. (nih.gov)
- To address the canonical pathway of NET formation-which involves generation of reactive oxygen species (ROS) and chromatin decondensation via histone citrullination by peptidyl arginine deiminase 4 (PAD4)-PMNs exposed to the medications were incubated with DPI (NADPH inhibitor), BB-Cl-amidine (PAD4 inhibitor) and muscarinic receptors antagonists. (nih.gov)
Ligand2
- The crystal structure of 3 reveals the presence of two isomers, cis or trans, depending on whether the terminal pyrazoles are coordinated at the same or at different sides of the approximate plane defined by the bridging bis-amidine ligand. (figshare.com)
- The clusters are produced by the reaction of the sodium salt of an amidine ligand with the gold precursor Au(THT)Cl in a (1:1) stoichiometry. (springernature.com)
Cationic1
- have suggested that DiC14 amidine cationic liposomes stimulate DCs via TLR-4. (medscape.com)
Compounds1
- Using the DTP COMPARE algorithm, compounds 1A and 1B were shown to correlate to each other at 77%, but failed to correlate with other benzimidazole based extended amidines previously synthesized in this laboratory suggesting they operate through a different biological mechanism. (asu.edu)
Ions1
- In the new study, the team concluded that electrifying bismuth films immersed in salt solutions containing imidazolium and amidine ions regulates chemical reactions that convert carbon dioxide into liquid fuel gasoline or the industrial chemical formic acid. (pfcstal.com)
Acids2
- Electrospray mass spectra of noncovalent complexes between amidines and various organic acids. (hw.ac.uk)
- The present invention relates to phenyl amidines of general formula (I), ##STR1## in which R.sup.1 to R.sup.5 are as defined in claim 1, their tautomers, their stereoisomers and their mixtures and their salts, especially their physiologically acceptable salts with inorganic or organic acids or bases also having valuable pharmacological properties, preferably aggregation-limiting effects, producing them. (justia.com)
Chemotherapeutic agents2
- This indicates that controlled release of Cl-amidine from P(3HB) microspheres may be effective in anti-cancer treatment, including in synergy with chemotherapeutic agents. (westminster.ac.uk)
- A potential new class of cancer chemotherapeutic agents has been synthesized by varying the 2 position of a benzimidazole based extended amidine. (asu.edu)
Linkage1
- The structure contains a unique four-amino acid macrocycle formed via a rare amidine linkage, C-methylation and a d-amino acid. (jic.ac.uk)
Amine1
- In addition, formation of an amidine product from the reaction of the amine with the ketenimine tautomer (the nitrile tautomer does not react with amine) supports the presence of the less stable tautomer in the equilibrium. (nih.gov)
Asymmetric2
- First, chiral amidine-based catalyst (ABC) HBTM-2 catalyzed an asymmetric cyclocondensation between in situ activated fluoroacetic acid and N-sulfonyl aldimines to give α-fluoro-β-lactams in highly enantioenriched form, achieving modest to excellent diastereoselectivities. (wustl.edu)
- Asymmetric α-alkylation of N′-tert-butanesulfinyl amidines. (elsevier.com)
Amino1
- Derivados de oxoácidos RnE(=O)OH en los que el grupo hidroxilo está sustituido por un grupo amino y el grupo oxo por =NR. Las amidinas incluyen carboxamidinas, sulfinamidinas y fosfinamidinas. (bvsalud.org)
Structural1
- The amidine structural motif within each core forms a bidentate interaction with a different aspartic acid of the catalytic diad. (proteopedia.org)
Inhibition3
- As Cl-amidine has been associated with anti-cancer effects, the Cl-amidine encapsulated microspheres were assessed for the inhibition of vascular endothelial growth factor (VEGF) expression in the mammalian breast cancer cell line SK-BR-3, including in the presence of the anti-proliferative drug rapamycin. (westminster.ac.uk)
- 11. Inhibition of PAD4-mediated NET formation by cl-amidine prevents diabetes development in nonobese diabetic mice. (nih.gov)
- The most potent and selective compound was the methylthio amidine analogue 9, which was more potent than l-nitroarginine with 185-fold selectivity for inhibition of neuronal NOS over endothelial NOS. (uthscsa.edu)
Formation1
- Hydralazine, but not procainamide, induced significant release of hydrogen peroxide in PMNs, and NET formation was inhibited by DPI and BB-Cl-amidine. (nih.gov)
Addition1
- The addition o f amidines to 1,2,3-triketohydrindenhydrat gives cyclic dihydroxyindenoimi-dazoles. (mpg.de)
Current1
- In the current study, P(3HB) microspheres with encapsulated Cl-amidine were produced in a size ranging from ~4−5 µm and characterized for surface morphology, porosity, hydrophobicity and protein adsorption, in comparison with empty P(3HB) microspheres. (westminster.ac.uk)
Activity1
- Vancomycin amidine turned out to have acceptable level of activity against vancomycin-resistant and -sensitive bacteria, yet there was room for improvement. (eurekalert.org)
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