AmidinesThioamides: Organic compounds containing the radical -CSNH2.Benzamidines: Amidines substituted with a benzene group. Benzamidine and its derivatives are known as peptidase inhibitors.Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.Molecular Structure: 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.Quinazolinones: Chemicals with two conjoined aromatic rings incorporating two nitrogen atoms and one of the carbons oxidized with a keto oxygen.Oxidative Coupling: The reaction of two molecular entities via oxidation usually catalyzed by a transition metal compound and involving dioxygen as the oxidant.Alkenes: Unsaturated hydrocarbons of the type Cn-H2n, indicated by the suffix -ene. (Grant & Hackh's Chemical Dictionary, 5th ed, p408)Acid Sensing Ion Channel Blockers: A subclass of sodium channel blockers that are specific for ACID-SENSING SODIUM CHANNELS.Catalysis: The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.Hydrocarbons, IodinatedDictionaries, MedicalDictionaries as Topic: Lists of words, usually in alphabetical order, giving information about form, pronunciation, etymology, grammar, and meaning.Dictionaries, ChemicalHeterocyclic Compounds: Ring compounds having atoms other than carbon in their nuclei. (Grant & Hackh's Chemical Dictionary, 5th ed)Furans: Compounds with a 5-membered ring of four carbons and an oxygen. They are aromatic heterocycles. The reduced form is tetrahydrofuran.Factor Xa: Activated form of factor X that participates in both the intrinsic and extrinsic pathways of blood coagulation. It catalyzes the conversion of prothrombin to thrombin in conjunction with other cofactors.Periodicals as Topic: A publication issued at stated, more or less regular, intervals.PubMed: A bibliographic database that includes MEDLINE as its primary subset. It is produced by the National Center for Biotechnology Information (NCBI), part of the NATIONAL LIBRARY OF MEDICINE. PubMed, which is searchable through NLM's Web site, also includes access to additional citations to selected life sciences journals not in MEDLINE, and links to other resources such as the full-text of articles at participating publishers' Web sites, NCBI's molecular biology databases, and PubMed Central.BooksPublishing: "The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.MEDLINE: The premier bibliographic database of the NATIONAL LIBRARY OF MEDICINE. MEDLINE® (MEDLARS Online) is the primary subset of PUBMED and can be searched on NLM's Web site in PubMed or the NLM Gateway. MEDLINE references are indexed with MEDICAL SUBJECT HEADINGS (MeSH).Serial Publications: Publications in any medium issued in successive parts bearing numerical or chronological designations and intended to be continued indefinitely. (ALA Glossary of Library and Information Science, 1983, p203)Electronic Mail: Messages between computer users via COMPUTER COMMUNICATION NETWORKS. This feature duplicates most of the features of paper mail, such as forwarding, multiple copies, and attachments of images and other file types, but with a speed advantage. The term also refers to an individual message sent in this way.Oximes: Compounds that contain the radical R2C=N.OH derived from condensation of ALDEHYDES or KETONES with HYDROXYLAMINE. Members of this group are CHOLINESTERASE REACTIVATORS.Amines: A group of compounds derived from ammonia by substituting organic radicals for the hydrogens. (From Grant & Hackh's Chemical Dictionary, 5th ed)Guanidine: A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.Guanidines: A family of iminourea derivatives. The parent compound has been isolated from mushrooms, corn germ, rice hulls, mussels, earthworms, and turnip juice. Derivatives may have antiviral and antifungal properties.Halogens: A family of nonmetallic, generally electronegative, elements that form group 17 (formerly group VIIa) of the periodic table.Stereoisomerism: 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)Hydrocarbons, HalogenatedMicrowaves: That portion of the electromagnetic spectrum from the UHF (ultrahigh frequency) radio waves and extending into the INFRARED RAYS frequencies.Green Chemistry Technology: Pollution prevention through the design of effective chemical products that have low or no toxicity and use of chemical processes that reduce or eliminate the use and generation of hazardous substances.Ionic Liquids: Salts that melt below 100 C. Their low VOLATILIZATION can be an advantage over volatile organic solvents.Anthraquinones: Compounds based on ANTHRACENES which contain two KETONES in any position. Substitutions can be in any position except on the ketone groups.Nylons: Polymers where the main polymer chain comprises recurring amide groups. These compounds are generally formed from combinations of diamines, diacids, and amino acids and yield fibers, sheeting, or extruded forms used in textiles, gels, filters, sutures, contact lenses, and other biomaterials.Distamycins: Oligopeptide antibiotics from Streptomyces distallicus. Their binding to DNA inhibits synthesis of nucleic acids.Netropsin: A basic polypeptide isolated from Streptomyces netropsis. It is cytotoxic and its strong, specific binding to A-T areas of DNA is useful to genetics research.Platinum Compounds: Inorganic compounds which contain platinum as the central atom.Rubiaceae: The Madder plant family of the order Rubiales, subclass Asteridae, class Magnoliopsida includes important medicinal plants that provide QUININE; IPECAC; and COFFEE. They have opposite leaves and interpetiolar stipules.GTP Cyclohydrolase: (GTP cyclohydrolase I) or GTP 7,8-8,9-dihydrolase (pyrophosphate-forming) (GTP cyclohydrolase II). An enzyme group that hydrolyzes the imidazole ring of GTP, releasing carbon-8 as formate. Two C-N bonds are hydrolyzed and the pentase unit is isomerized. This is the first step in the synthesis of folic acid from GTP. EC 3.5.4.16 (GTP cyclohydrolase I) and EC 3.5.4.25 (GTP cyclohydrolase II).Riboflavin: Nutritional factor found in milk, eggs, malted barley, liver, kidney, heart, and leafy vegetables. The richest natural source is yeast. It occurs in the free form only in the retina of the eye, in whey, and in urine; its principal forms in tissues and cells are as FLAVIN MONONUCLEOTIDE and FLAVIN-ADENINE DINUCLEOTIDE.Encyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Biopterin: A natural product that has been considered as a growth factor for some insects.Pterins: Compounds based on 2-amino-4-hydroxypteridine.AminohydrolasesPimelic Acids: A group of compounds that are derivatives of heptanedioic acid with the general formula R-C7H11O4.AmidohydrolasesDiaminopimelic AcidMedlinePlus: NATIONAL LIBRARY OF MEDICINE service for health professionals and consumers. It links extensive information from the National Institutes of Health and other reviewed sources of information on specific diseases and conditions.Lysine: An essential amino acid. It is often added to animal feed.Carbon: A nonmetallic element with atomic symbol C, atomic number 6, and atomic weight [12.0096; 12.0116]. It may occur as several different allotropes including DIAMOND; CHARCOAL; and GRAPHITE; and as SOOT from incompletely burned fuel.

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)

Abstract. Copper-catalyzed cross-coupling reactions of amidine salts with aryl iodides give monoarylated amidines in good yields under ligand-free conditions. DMF was the superior solvent for the N-arylation of benzamidines, while MeCN was used in the formation of N-aryl amidines in good yield.. ...
Palladium-catalysed coupling between aryl- or heteroaryl-bromides, alkoxides, aryloxides or thioalkoxides. and isocyanides gives aryl-imidates and -thioimidates in high yield. Amidines can be synthesised in a one-pot procedure via imidates.. Full text not available from this repository.. ...
GRAPHICS] Phosphoryl azide was successfully employed as an efficient reacting partner in the Cu-catalyzed three-component reaction with 1-alkynes and amines to produce the corresponding phosphoryl amidines in high yields. A range of fruitful applicability of the produced amidines was also demonstrated such as an alkoxide exchange and asymmetric alpha-alkylation of optically active BINOL-derived amidines ...
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Trimethylsilyl-transient protection successfully allowed the use of lithium hexamethyldisilazane to prepare benzimidazole (BI) and 4-azabenzimidazole (azaBI) amidines from nitriles in 58-88% yields. This strategy offers a much better choice to prepare BI/azaBI amidines than the lengthy, low-yielding Pinner reaction. Synthesis of aza/benzimidazole rings from aromatic diamines and aldehydes was affe ...
Trimethylsilyl-transient protection successfully allowed the use of lithium hexamethyldisilazane to prepare benzimidazole (BI) and 4-azabenzimidazole (azaBI) amidines from nitriles in 58-88% yields. This strategy offers a much better choice to prepare BI/azaBI amidines than the lengthy, low-yielding Pinner reaction. Synthesis of aza/benzimidazole rings from aromatic diamines and aldehydes was affe ...
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New acetamidines structurally related to N-(3-(aminomethyl)benzyl)acetamidine (1, W1400) were designed as inhibitors of inducible nitric oxide synthase (iNOS). Six compounds were found to be selective for iNOS over endothelial nitric oxide synthase (eNOS), and among them, the most active and selecti …
Grundy, Joanna, Coles, Martyn P and Hitchcock, Peter B (2004) Ambiphilic Ligands from the 1,4-benzenebis(amidine) Framework. New Journal of Chemistry, 28 (10). 1195 - 1197. ISSN 1144-0546 Full text not available from this repository ...
benzyl 3-(aminomethyl)piperidine-1-carboxylate 315717-76-1 route of synthesis, benzyl 3-(aminomethyl)piperidine-1-carboxylate chemical synthesis methods, benzyl 3-(aminomethyl)piperidine-1-carboxylate synthetic routes ect.
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 ...
Luxol fast blue (Methasol fast blue) is a copper phtalocyanine dye which is employed in myelin demonstration and can be combined with Nissl staining, PAS or van Gieson.. This technique allows easy differentiation of the Luxol Fast Blue. ...
This invention provides a coating composition which utilizes a free radical initiator and an organic tintability additive which remains substantially unpolymerized even after the remainder of the coating composition is cured. Superior tintability and adhesion to polycarbonate makes this coating particularly suitable for making tinted opthalmic lenses.
73425-53-3 - CCNHJBDXFBSFAA-UHFFFAOYSA-N - Thiopyrano(2,3-b)indole, 2,3,4,9-tetrahydro-4-(aminomethyl)-6-methyl- - Similar structures search, synonyms, formulas, resource links, and other chemical information.
chemBlink provides information about CAS # 144288-50-6, 3-Amino-2-pyridinemethanamine, 3-Amino-2-(aminomethyl)pyridine, molecular formula: C6H9N3.
(S,R,S)-AHPC-C8-NH2 dihydrochloride (VH032-C8-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1. - Mechanism of Action & Protocol.
CP 31398 dihydrochloride, p53 stabilizing agent. Stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53. Inhibits growth of small human tumor xenografts in vivo.
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MRT68921 dihydrochloride is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. - Mechanism of Action & Protocol.
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Microwave reactions of primary and secondary amines with imidoylbenzotriazoles 6a-w gave diversely substituted amidines 7a-Aa in 76-94% yields. Convenient preparations of a variety of amides 5a-Ab (87-96%) and imidoylbenzotriazoles 6a-w (56-95%) have also been developed using microwave irradiation under mild conditions and short reaction times. These results demonstrate further the advantages of microwave synthesis and introduce a new application of imidoylbenzotriazoles in the preparation of polysubstituted amidines.
Amidines bearing simple alkenes undergo aminal radical cyclisation upon treatment with SmI2. The mild, reductive electron transfer process delivers medicinally-relevant, polycyclic quinazolinone derivatives in good to excellent yield and typically with complete diastereocontrol.
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Looking for online definition of amidine in the Medical Dictionary? amidine explanation free. What is amidine? Meaning of amidine medical term. What does amidine mean?
A fast and convenient synthesis of aryl amidines starting from carboxylic acids and cyanamides is reported. The reaction was achieved by palladium(II)-catalysis in a one-step microwave protocol using [Pd(O2 CCF3 )2 ], 6-methyl-2,2-bipyridyl and trifluoroacetic acid (TFA) in N-methylpyrrolidinone (NMP), providing the corresponding aryl amidines in moderate to excellent yields ...
BioAssay record AID 159272 submitted by ChEMBL: Percent inhibition of 2,2-azobis(2-amidinopropane)dihydrochloride induced decay of (R)-phycoerythrin fluorescence emission.
BioAssay record AID 724354 submitted by ChEMBL: Antioxidant activity assessed as inhibition of AAPH-induced linoleic acid lipid peroxidation at 100 uM by spectrophotometric analysis.
The protein arginine deiminases (PADs), and in particular PAD4, have emerged as potential therapeutic targets for the treatment of rheumatoid arthritis (RA). In this review, evidence linking dysregulated PAD activity to the onset and progression of RA is presented, and the potential role of such aberrant activity in other human diseases, such as multiple sclerosis and cancer, is discussed. The known physiological roles of the PADs, particularly PAD4, and current knowledge regarding PAD structure, catalysis and inhibition are also described.
YW3-56 YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor with inhibitory activity against PAD2 (IC50=0.5-1 uM) and PAD4 (IC50=1-2 uM), inhibits U2OS cancer cell growth with IC50 of 2.5 uM.. ...
Page contains details about formamidinium lead iodide/methylammonium lead iodide-based perovskite solar cell . It has composition images, properties, Characterization methods, synthesis, applications and reference articles : nano.nature.com
2,693,468 Patented Nov, 2, 1954 hce CONTAINING COMPQUND AND METHOD OF P E ARING. AM flha l s air, J W s Groves MQ-J assign: t Petro i e Co p ti n, @QFHQEflfiQll of D lawar No Drawing, Application February 28, 1952 Serial No. 274,075 Claims. (Cl. 2601-2564) This invention relates to a new class of chemical compounds, namely, certain waxdike and wax-derived compositions containing basic nitrogen groups, and to methods of preparing these compositions. In its broadest aspect, my invention is concerned with new wax-like basic nitrogen compounds derived by reaction of high molecular weight oxidized waxes, of the kind more fully described below, and certain polyamines. The products will usually consist of a mixture of homologous compounds comprising aminoamidcs and cyclic amidines, as well as some unreacted wax employed as starting material in the preparation of the oxidized wax reactant, but under the preferred conditions of reaction recited herein will contain substantial amounts of compounds ...
INTRODUCTION. The name amidoxime was first used by Tiemann1, who identified the structure of this class of compounds in 1884. Amidoximes constitute an important class of compound 2,3 in their own right and have been employed for the synthesis 2-6 of a variety of valuable compounds. Their importance in chemistry, along with their rich biology, makes amidoximes an attractive target for medicinal chemists, biochemists and biologists7.. Amidoximes have exhibited important biological activities, for example, as antitripanocidics8, antituberculotics9,10, hypotensives and antiarrhythmics11, antibacterials and fungicidals12. Amidoxime have been tested for pharmacological properties and have been found to be useful as local anaesthetics13, fibrinogen receptor antagonists14, and as antileishmanial agents15. A number of amidoximes have already been used as prodrugs for amidines16, or are currently being used in clinical trials7. Many recent pharmaceutical applications have been enriched, with some of their ...
Kirilov G.K.; Belyakov S.V.; Kirilova E.M.; Gerbreder V. Structural and luminescence properties of substituted benzanthronyl amidines and its complexes with transition metals. Conference Programme and Book of Abstracts, 11th Conference on Methods and Applications of Fluorescence; August: P.28. Budapest, Hungary, 2009; 86 ...
reference: Protein Arginine Deiminase 2 Binds Calcium in an Ordered Fashion: Implications for Inhibitor Design., Slade DJ, Fang P, Dreyton CJ, Zhang Y, Fuhrmann J, Rempel D, Bax BD, Coonrod SA, Lewis HD, Guo M, Gross ML, Thompson PR, ACS Chem Biol. 2015 Jan 26. PMID: 25621824 ...
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The main focus of research in the Birman group is on the de novo design of asymmetric catalysts and reagents. As part of this effort, they have developed Amidine-Based Catalysts, or ABCs, and demonstrated their high enantioselectivity in many asymmetric acyl transfer reactions. The versatility, accessibility, and ease of structural modification of ABCs have attracted the interest of a number of other research groups worldwide, which has led to further expansion of their synthetic utility ...
N-(2-amino-5-fluorobenzyl)-4-(N-(pyridine-3-acrylyl)aminomethyl)benzamide: an antineoplastic agent and histone deacetylase inhibitor; structure in first source
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Ono has cloned and expressed the gene for interleukin-4. The molecule, which stimulates B-cells and T-cells in vitro, was being studied preclinically as an
1LHG: Kinetic and crystallographic studies of thrombin with Ac-(D)Phe-Pro-boroArg-OH and its lysine, amidine, homolysine, and ornithine analogs.
Mannomustine administered as the dihydrochloride is carcinogenic in mice following its intraperitoneal injection, producing an increased incidence of leukaemia and a dose-related increase in the incidence of lung tumours. ...
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... specifically in cyclic amidines. The systematic name of this enzyme class is GTP 7,8-8,9-dihydrolase (diphosphate-forming). ...
3.5.4: Cyclic amidines/. Aminohydrolases. *Guanine deaminase. *Adenosine deaminase. *AMP deaminase. *Inosine monophosphate ...
3.5.4: Cyclic amidines/. Aminohydrolases. *Guanine deaminase. *Adenosine deaminase. *AMP deaminase. *Inosine monophosphate ...
Esters Amidines Roger, Robert; Neilson, Douglas G. (1961). "The Chemistry of Imidates". Chemical Reviews. 61 (2): 179-211. doi: ... They can be hydrolyzed to give esters and by an analogous process react with amines (including ammonia) to form amidines. ...
In these schemes, amidines can be directly converted to diazirines by hypohalite oxidation. This reaction yields a halogenated ... Graham, W. H. (1965-10-01). "The Halogenation of Amidines. I. Synthesis of 3-Halo- and Other Negatively Substituted Diazirines1 ...
"Amidines Derived from Pt(IV)-Mediated Nitrile−Amino Alcohol Coupling and Their Zn(II)-Catalyzed Conversion into Oxazolines". ... preceding via an intermediate amidine.[19][20] Limited research has been done into identifying alternative solvents or ...
Aromatic Amidines as Competitive Inhibitors of Trypsin". The Journal of Biochemistry. 69 (5): 893-899. doi:10.1093/ ...
3.5.4: Cyclic amidines/. Aminohidrolaze. *Guanin deaminaza. *Adenozin deaminaza. *AMP deaminaza. *Inozin monofosfat sintaza ...
... has been reported to reduce amidoximes to amidines. MOCOS Anantharaman V, Aravind L (January 2002). "MOSC domains: ...
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 ...
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. ...
Amidine protecting groups for oligonucleotide synthesis". J. Am. Chem. Soc. 108 (8): 2040-2048. doi:10.1021/ja00268a052. Guzaev ...
Amidine protecting groups for oligonucleotide synthesis". J. Am. Chem. Soc. 108: 2040. doi:10.1021/ja00268a052. Sinha, N. D.; ...
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 With water to form a esters. ...
Increasingly important in organic synthesis, these include the phosphazenes, amidines, and guanidines. Other organic compounds ...
It binds free amino groups at pH range 7.0-10.0 to form amidine bonds. DMP is used mainly as bifunctional coupling reagent to ...
... to yield a branched amidine intermediate. To obtain the final product macrocycle, macrolactamization of the amidine-containing ... To obtain the amidine linkage, a tripeptide intermediate was coupled to a phthaloyl-protected thioamide via mercury-mediated ... The resulting macrocycle was obtained as a racemic mixture at the amidine linkage. The full synthetic scheme may be viewed ... The structure of bottromycin contains a macrocyclic amidine as well as a thiazole ring. The absolute stereochemistry at several ...
It belongs to the class of pyrrole-amidine antibiotics. Netropsin binds to the minor groove of AT-rich sequences of double ...
It is an amidine base used in organic synthesis. A related compound with related functions is 1,8-diazabicyclo[5.4.0]undec-7- ...
... is an amidine which serves as a serotonin inhibitor. This agent is prepared by alkylation of 3-methoxyphenol (m- ...
Quantum-chemical calculations concerning the spontaneous rearrangement of the adduct into ring-contracted amidines". ...
Intermediate arylamidine 2 is prepared by HCl-catalyzed addition of aniline to the nitrile function of 4-cyanothiazole (1). The ... amidine (2) is then converted to its N-chloro analog 3 with sodium hypochlorite (NaOCl). Upon treatment with base, this ...
This enzyme belongs to the family of lyases, specifically amidine lyases. The systematic name of this enzyme class is ...
This enzyme belongs to the family of lyases, specifically amidine lyases. The systematic name of this enzyme class is DNA-4,6- ...
Amidine-lyases Kasutatud 23.10.2016 (inglise) *↑ 11,0 11,1 Craik, C. S. et al., (2011). Proteases as therapeutics. Biochem J., ...
Amidines are a class of oxoacid derivatives. The oxoacid from which an amidine is derived must be of the form RnE(=O)OH, where ... Examples of amidines include: DBU diminazene benzamidine Pentamidine Paranyline The most common way to make primary amidines is ... treatment of this with ammonia then completes the conversion to the amidine. Amidines are much more basic than amides and are ... as they are the most commonly encountered type of amidine in organic chemistry. The simplest amidine is formamidine, HC(=NH)NH2 ...
Amidines Definition Derivatives of oxoacids RnE(=O)OH in which the hydroxy group is replaced by an amino group and the oxo ...
... Muhammad Abdul Qadir,1 Mahmood Ahmed, ... Muhammad Abdul Qadir, Mahmood Ahmed, Hina Aslam, Sadia Waseem, and Muhammad Imtiaz Shafiq, "Amidine Sulfonamides and Benzene ...
Amidines bearing simple alkenes undergo aminal radical cyclisation upon treatment with SmI2. The mild, reductive electron ... Reductive cyclisations of amidines involving aminal radicals H. Huang, R. W. Adams and D. J. Procter, Chem. Commun., 2018, 54, ... Amidines bearing simple alkenes undergo aminal radical cyclisation upon treatment with SmI2. The mild, reductive electron ...
Copper-catalyzed cross-coupling reactions of amidine salts with aryl iodides give monoarylated amidines in good yields under ... DMF was the superior solvent for the N-arylation of benzamidines, while MeCN was used in the formation of N-aryl amidines in ... Ligand-Free Copper-Catalyzed Arylation of Amidines. Michelle Cortes-Salva, Corey Garvin and Jon C. Antilla*. *Department of ...
The oxalic amidine N,N′-dimethyl-N,N′-diphenyl-1,2-bis[4-tolylimino]ethane-1,2-diamine was used to synthesise a chloridozinc ... Oxalic Amidines - Protonation Studies and Activity in Lactide Polymerisation† Authors. *. Ines dos Santos Vieira,. *Fakultät ...
C. F. Silva, M. B. Meuser, E. M. De Souza et al., "Cellular effects of reversed amidines on Trypanosoma cruzi," Antimicrobial ... E. M. De Souza, P. B. da Silva, A. S. Nefertiti et al., "Trypanocidal activity and selectivity in vitro of aromatic amidine ... A. Daliry, M. Munde, M. Q. Pires et al., "The trypanocidal activity of amidine compounds does not correlated with their binding ... previously known as reversed amidines, have extraordinary activity against both Leishmania [71-73] and T. cruzi [52, 53, 55, 56 ...
... amidine explanation free. What is amidine? Meaning of amidine medical term. What does amidine mean? ... Looking for online definition of amidine in the Medical Dictionary? ... Amidine , definition of amidine by Medical dictionary https://medical-dictionary.thefreedictionary.com/amidine ... amidine. Also found in: Dictionary, Encyclopedia, Wikipedia. am·i·dine. (ami-dēn), The monovalent radical -C(NH)-NH2. ...
Amidine systems are intermediate in structure between tertiary amines and quaternary compounds, at least as regards ionization ... Amidines (guanidine, formamidine, and acetamidine) were introduced as substitutes for the cationic heads present in atropine, ... Thus, amidine moieties are effective bioisosteric substitutes for conventional cationic heads present in antimuscarinic agents ... Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric ...
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity ...
Antibacterial action of some aromatic amines, amidines, amidoximes, guanidines and diguanidines. A. T. Fuller ... Antibacterial action of some aromatic amines, amidines, amidoximes, guanidines and diguanidines Message Subject (Your Name) has ...
Amidines can be synthesised in a one-pot procedure via imidates.. imidate, thioimidate, amidine, palladium homogeneous ... Palladium-catalysed synthesis of imidates, thioimidates and amidines from aryl halides. Palladium-catalysed coupling between ... Keywords: imidate, thioimidate, amidine, palladium homogeneous catalysis multicomponent reactionscarbonylation, derivatives ... Palladium-catalysed synthesis of imidates, thioimidates and amidines from aryl halides. ...
Cl-amidine is an inhibitor of protein arginine deiminases (PAD, IC50s = 0.8, 6.2, and 5.9 µM for PAD1, PAD3, and PAD4 in vitro ... Product information "Cl-Amidine (trifluoroacetate salt)" Cl-amidine is an inhibitor of protein arginine deiminases (PAD, IC50s ... Cl-amidine is cytotoxic to HL-60, MCF7, and HT-29 cancer cell lines (IC50s = 0.25, 0.05 and 1 µM, respectively). In a collagen- ... Cl-amidine is an inhibitor of protein arginine deiminases (PAD, IC50s = 0.8, 6.2, and 5.9 µM for... more ...
The private veterinary market is divided between products only effective against ticks (amidines) and those effective against ... Bardosh, K., Waiswa, C. & Welburn, S.C. Conflict of interest: use of pyrethroids and amidines against tsetse and ticks in ... The sale of acaricide varied by price, dilution rate and availability (see Table 3). Amidine-based products (which were ... Conflict of interest: use of pyrethroids and amidines against tsetse and ticks in zoonotic sleeping sickness endemic areas of ...
... of microwave synthesis and introduce a new application of imidoylbenzotriazoles in the preparation of polysubstituted amidines. ... Microwave reactions of primary and secondary amines with imidoylbenzotriazoles 6a-w gave diversely substituted amidines 7a-Aa ... Efficient microwave access to polysubstituted amidines from imidoylbenzotriazoles.. *. Alan R. Katritzky, Chunming Cai, Sandeep ... Microwave reactions of primary and secondary amines with imidoylbenzotriazoles 6a-w gave diversely substituted amidines 7a-Aa ...
Mesh term Amidines. Browse to parent terms:. Organic Chemicals. Description. Derivatives of oxoacids RnE(=O)OH in which the ... Amidines include carboxamidines, sulfinamidines and phosphinamidines.. Browse to child terms:. Benzamidines. Chlorphenamidine. ...
Chiral ferrocenyl amidines as modular ligands for applications in asymmetric catalysis. * Mendeley ... ASYMMETRISCHE KATALYSE (CHEMISCHE REAKTIONEN); AMIDINE (ORGANISCHE CHEMIE); CYCLOPENTADIENYLKOMPLEXE (KOMPLEXCHEMIE); ... ORGANISCHE SYNTHESE (CHEMIE); ASYMMETRIC CATALYSIS (CHEMICAL REACTIONS); AMIDINES (ORGANIC CHEMISTRY); CYCLOPENTADIENYL ...
Reductive cyclisations of amidines involving aminal radicals. Research output: Contribution to journal › Article ... Amidines bearing simple alkenes undergo aminal radical cyclisation upon treatment with SmI2. The mild, reductive electron ... HomeResearchResearch ExplorerPublicationsReductive cyclisations of amidines involving aminal radicals ...
Novel polyamide amidine anthraquinone platinum(II) complexes for enhancing DNA binding and tumour penetration. ...
Synthesis of cyclic amidines pka. November 23, 2018. MiaArgumentative Essays Das, d. after synthesis of cyclic amidines pka ... amidines pka amidines suitcase size guide liters to cubic inches followed by spontaneous cyclization to yield cyclic amidines, ... synthesis of cyclic amidines pka synthesis of medium-ring bicyclic diamines by the alkylation and cleavage of cyclic amidines. ... is a hereditary neuromuscular disease synthesis of cyclic amidines pka marked by the progressive weakness and muscle loss, with ...
... adhesives from a plurality of surfaces through the use of an aqueous or non-aqueous basic organic solvent and/or an amidine, ... Amidine Solvents. In an aspect, an amidine solvent is included in the label removing composition. An amidine solvent is a non- ... Amidine Solvents 1-20 5-20 7-15 Additional Solvents 0.01-15 0.1-15 5-15 Surfactants 0-50 5-40 10-30 Water 5-90 10-80 20-70 ... Amidine Solvents 30-70 40-70 50-65 Additional Solvents 5-50 10-50 20-40 Surfactants 5-50 5-25 10-20 Sodium Hydroxide (caustic) ...
Interestingly, Cl-amidine drives apoptosis of inflammatory cells in vitro and in vivo, providing a mechanism by which Cl- ... In total, these data help validate the PADs as therapeutic targets for the treatment of IBD and further suggest Cl-amidine as a ... Results are consistent with this hypothesis, as demonstrated by the finding that Cl-amidine treatment, both prophylactic and ... Cl-amidine), could suppress colitis in a dextran sulfate sodium mouse model. ...
... Chemical Society Reviews. 42 (17): pp. 7326-7334. ... This mini-review describes basic features and applications of small molecules and macromolecules containing amidine, and to a ...
Supplier and Exporter of Dabigatran Amidine Impurity in Mumbai, Maharashtra, India. ... Dabigatran Amidine Impurity. *3-({2-[(4-Carbamimidoyl-phenylamino)-methyl]-1-methyl-1H-benzoimidazole ...
Tetrodotoxin (TTX) is a potent neurotoxin. Its name derives from Tetraodontiformes, an order that includes pufferfish, porcupinefish, ocean sunfish, and triggerfish; several of these species carry the toxin. Although tetrodotoxin was discovered in these fish and found in several other aquatic animals (e.g., in blue-ringed octopuses, rough-skinned newts, and moon snails), it is actually produced by certain infecting or symbiotic bacteria like Pseudoalteromonas, Pseudomonas, and Vibrio as well as other species found in the animals ...
  • It has been known for some time that amidine and guanidine derivatives will inhibit C-mediated hemolysis (i.e. (thefreedictionary.com)
  • Amidines (guanidine, formamidine, and acetamidine) were introduced as substitutes for the cationic heads present in atropine, scopolamine, and corresponding quaternary derivatives. (nih.gov)
  • This mini-review describes basic features and applications of small molecules and macromolecules containing amidine, and to a lesser extent, guanidine functional groups. (edu.au)
  • Three PFPA homopolymers of different molecular weights were reacted with the commercially available amidine and guanidine species histamine (HIS) dihydrochloride and L-arginine methyl ester (ARG) dihydrochloride in the presence of S-methyl methanethiosulfonate to yield, quantitatively, the corresponding amidine and guanidine-based acrylamido homopolymers. (edu.au)
  • Amidine systems are intermediate in structure between tertiary amines and quaternary compounds, at least as regards ionization and electronic properties, but differ from the latter in shape (planar not tetrahedral). (nih.gov)
  • Microwave reactions of primary and secondary amines with imidoylbenzotriazoles 6a-w gave diversely substituted amidines 7a-Aa in 76-94% yields. (semanticscholar.org)
  • They can be hydrolyzed to give esters and by an analogous process react with amines (including ammonia) to form amidines. (wikipedia.org)
  • This enzyme belongs to the family of hydrolases , those acting on carbon-nitrogen bonds other than peptide bonds, specifically in cyclic amidines. (wikipedia.org)
  • Copper-catalyzed cross-coupling reactions of amidine salts with aryl iodides give monoarylated amidines in good yields under ligand-free conditions. (organic-chemistry.org)
  • DMF was the superior solvent for the N -arylation of benzamidines, while MeCN was used in the formation of N -aryl amidines in good yield. (organic-chemistry.org)
  • The reaction was achieved by palladium(II)-catalysis in a one-step microwave protocol using [Pd(O2 CCF3 )2 ], 6-methyl-2,2'-bipyridyl and trifluoroacetic acid (TFA) in N-methylpyrrolidinone (NMP), providing the corresponding aryl amidines in moderate to excellent yields. (mendeley.com)
  • With only two freely rotatable bonds, molecular modeling suggests that one amidine group is positioned into the S1 pocket, forming hydrogen bonds with the side chain of Asp189, similar to other amidine-based inhibitors, with the second benzamidine positioned into the S4 pocket in a position to form strong cation-pi bonding with the S4 aryl cage. (researchwithrutgers.com)
  • Due to interest in the coordination chemistry of formamidines, the non-symmetric amidine ligands PhNC(Me)NHPri, PhNC(Et)NHPri, and (2,4,6-Me3C6H2)NC(Me)NHPri, have been synthesized, and their reaction with Os3(CO)10(MeCN)2 has been investigated. (unt.edu)
  • When the parent oxoacid is a carboxylic acid, the resulting amidine is a carboxamidine or carboximidamide (IUPAC name), and has the following general structure: Carboxamidines are frequently referred to simply as amidines, as they are the most commonly encountered type of amidine in organic chemistry. (wikipedia.org)
  • Because epithelial cell DNA damage associated with colitis is at least in part a result of an oxidative burst from overactive leukocytes, we tested the hypothesis that Cl-amidine can inhibit leukocyte activation, as well as subsequent target epithelial cell DNA damage in vitro and in vivo. (aspetjournals.org)
  • In vitro studies indicated that Cl-amidine may act as a tumor suppressor by upregulating miR-16, a putative tumor suppressor miRNA with cell cycle targets, and causing G1 cell cycle arrest. (sc.edu)
  • Because colitis is defined as inflammation of the colon associated with infiltration of white blood cells that release free radicals and citrullination is an inflammation-dependent process, we asked whether Cl-amidine has antioxidant properties. (aspetjournals.org)
  • For a mechanistic study of Cl-amidine, we explored the idea that Cl-amidine may be preventing the citrullination and/or hyperactivity of DNA methyltransferases (DNMTs). (sc.edu)
  • We have previously reported that non-symmetrical furan amidines are potent inhibitors of NQO2 and here novel analogues are evaluated. (aston.ac.uk)
  • Results are consistent with this hypothesis, and because DNA damage is a procancerous mechanism, our data predict that Cl-amidine will not only suppress colitis, but we hypothesize that it may prevent colon cancer associated with colitis. (aspetjournals.org)
  • Catalytic, enantioselective N-acylation of lactams and thiolactams using amidine-based catalysts. (sigmaaldrich.com)
  • A new method for catalytic nonenzymatic kinetic resolution of α-substituted alkanoic acids has been developed, which relies on their activation with DCC followed by enantioselective alcoholysis of the intermediate symm-anhydrides in the presence of the amidine-based catalyst homobenzotetramisole (HBTM). (sigmaaldrich.com)
  • Amidines are much more basic than amides and are among the strongest uncharged/unionized bases. (wikipedia.org)
  • The furan ring has been changed to other heterocycles (imidazole, N-methylimidazole, oxazole, thiophene) and the amidine group has been replaced with imidate, reversed amidine, N-arylamide and amidoxime to probe NQO2 activity, improve solubility and decrease basicity of the lead furan amidine. (aston.ac.uk)
  • Fingerprint Dive into the research topics of 'Asymmetric α-alkylation of N′-tert-butanesulfinyl amidines. (elsevier.com)
  • These amidines are electrically neutral in undisturbed water, but when carbon dioxide bubbles through, the compounds transform into amidinium bicarbonate salts that act as surfactants. (thefreedictionary.com)
  • Results are consistent with this hypothesis, as demonstrated by the finding that Cl-amidine treatment, both prophylactic and after the onset of disease, reduced the clinical signs and symptoms of colitis, without any indication of toxic side effects. (umassmed.edu)
  • Our results showed that in the AOM/DSS murine model of UC-associated CRC, Cl-amidine significantly inhibited tumorigenesis, further supporting our hypothesis. (sc.edu)
  • Asymmetric α-alkylation of N′-tert-butanesulfinyl amidines. (elsevier.com)
  • The observed structure-activity relationship for the furan-amidine series with NQO2 was rationalized by preliminary molecular docking and binding mode analysis. (aston.ac.uk)
  • In a collagen-induced mouse model of inflammatory arthritis, Cl-amidine dose-dependently decreases the citrulline content in serum and joints and reduces the development of IgG autoantibodies. (biomol.com)
  • Inducible nitric oxide synthase, an inflammatory marker, was also downregulated in macrophages by Cl-amidine. (aspetjournals.org)
  • Asymmetric N-acylation promoted by amidine-based catalysts, particularly Cl-PIQ 2 and BTM 3, provides a convenient method for the kinetic resolution of these valuable compounds and ofte. (sigmaaldrich.com)
  • As part of this effort, they have developed Amidine-Based Catalysts, or ABCs, and demonstrated their high enantioselectivity in many asymmetric acyl transfer reactions. (sigmaaldrich.com)
  • We showed that Cl-amidine effectively reduced inflammation, oxidative stress produced by activated leukocytes, and DNA damage. (sc.edu)
  • Next, we tested the efficacy of Cl-amidine in the HCT116 colon cancer cell line and the Azoxymethane (AOM)/Dextran Sulfate Sodium (DSS) murine model of UC. (sc.edu)
  • In total, these data help validate the PADs as therapeutic targets for the treatment of IBD and further suggest Cl-amidine as a candidate therapy for this disease. (umassmed.edu)
  • 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. (biomedcentral.com)
  • At these pH values, the nucleophilic attack of an R-N[H.sub.on one of the two outer backbone carbon atoms of dimethyl pimelimidate produces a tetrahedral intermediate that splits into the amidine link and methanol. (thefreedictionary.com)
  • Here we show that colitis induced with azoxymethane via intraperitoneal injection + 2% dextran sulfate sodium in the drinking water is suppressed by Cl-amidine (also given in the drinking water). (aspetjournals.org)