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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.2289-75-0, Name is 4,5-Dimethylthiazol-2-amine, molecular formula is C5H8N2S. In a Patent,once mentioned of 2289-75-0, Recommanded Product: 4,5-Dimethylthiazol-2-amine

Isothiourea derivatives and their use in medicine, particularly in the treatment of conditions where there is an advantage in inhibiting nitric oxide synthase, pharmaceutical formulations comprising the same and processes for the preparation thereof are disclosed.

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Reference:
Thiazole | C3H4999NS – PubChem,
Thiazole | chemical compound | Britannica

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Peptide deformylase (PDF) is a prokaryotic metalloenzyme that is essential for bacterial growth and is a new target for the development of antibacterial agents. All previously reported PDF inhibitors with sufficient antibacterial activity share the structural feature of a 2-substituted alkanoyl at the P1? site. Using a combination of iterative parallel synthesis and traditional medicinal chemistry, we have identified a new class of PDF inhibitors with N-alkyl urea at the P1? site. Compounds with MICs of ?4 mug/ml against gram-positive and gram-negative pathogens, including Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae, have been identified. The concentrations needed to inhibit 50% of enzyme activity (IC50s) for Escherichia coli Ni-PDF were ?0.1 muM, demonstrating the specificity of the inhibitors. In addition, these compounds were very selective for PDF, with IC50s of consistently >200 muM for matrilysin and other mammalian metalloproteases. Structure-activity relationship analysis identified preferred substitutions resulting in improved potency and decreased cytotoxity. One of the compounds (VRC4307) was cocrystallized with PDF, and the enzyme-inhibitor structure was determined at a resolution of 1.7 A. This structural information indicated that the urea compounds adopt a binding position similar to that previously determined for succinate hydroxamates. Two compounds, VRC4232 and VRC4307, displayed in vivo efficacy in a mouse protection assay, with 50% protective doses of 30.8 and 17.9 mg/kg of body weight, respectively. These N-alkyl urea hydroxamic acids provide a starting point for identifying new PDF inhibitors that can serve as antimicrobial agents.

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Reference:
Thiazole | C3H4991NS – PubChem,
Thiazole | chemical compound | Britannica

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In this study, we aimed at the synthesis of new 2-((5-substituted-4- methylthiazol-2-yl)amino)-2-oxoethyl 4- substitutedpiperazine-1-carbodithioate derivatives and their antibacterial, antifungal, antioxidant and AChE inhibitory evaluations. A set of fifteen new compounds of 2-((5-substituted-4- methylthiazol-2-yl)amino)-2-oxoethyl 4-substitutedpiperazine-1-carbodithioate derivatives were synthesised by reacting 2-chloro-N-(5-substituted-4- methylthiazole-2- yl)acetamide derivatives and sodium salts of appropriate N-substitutedpiperazine dithiocarbamic acids in acetone. The chemical structures of the compounds were elucidated by IR, 1H-NMR, 13C-NMR, MS spectral data and elemental analysis. The antibacterial and antifungal activities of the synthesised derivatives were tested against Gram (+), Gram (-) bacteria and yeasts such as Salmonella typhimurium, Staphylococcus epidermidis, Staphylococcus aureus, Escherichia coli, Candida albicans, Candida utilis, Candida tropicalis, Candida krusei and Candida glabrata using a microbroth dilution technique. Antimicrobial results showed that the compounds displayed minimum inhibitory concentrations in the range of 15.62-4000 mug/mL. Antioxidant activity of the synthesised derivatives was measured by scavenging activity against DPPH (2,2-Diphenyl-1-picrylhydrazyl) radical and qualitative ABTS (2,2?-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) free radical scavenging assay and it was found that the compounds showed antioxidant activity. AChE inhibitory activity of the synthesised derivatives was tested against Donepezil for their ability to inhibit acetylcholinesterase (AChE) using a modification of Ellman’s spectrophotometric method. However, no significant inhibitory activity was observed.

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Thiazole | C3H5000NS – PubChem,
Thiazole | chemical compound | Britannica

Discovery of 4,5-Dimethylthiazol-2-amine

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2-Fluoro-5-(2-hydroxyethyl)-4-methylthiazole and 5-(2-fluoroethyl)-4-methylthiazole have been prepared and the latter converted into a fluoro-analogue of thiamine.All three compounds show bacteriostatic activity against E. coli.

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Reference:
Thiazole | C3H5042NS – PubChem,
Thiazole | chemical compound | Britannica

Top Picks: new discover of 4,5-Dimethylthiazol-2-amine

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In this study, a new series of more than 60 quinoline derivatives has been synthesized and evaluated against Mycobacterium tuberculosis (H37Rv). Apart from the SAR exploration around the initial hits, the optimization process focused on the improvement of the physicochemical properties, cytotoxicity, and metabolic stability of the series. The best compounds obtained exhibited MIC values in the low micromolar range, excellent intracellular antimycobacterial activity, and an improved physicochemical profile without cytotoxic effects. Further investigation revealed that the amide bond was the source for the poor blood stability observed, while some of the compounds exhibited hERG affinity. Compound 83 which contains a benzoxazole ring instead of the amide group was found to be a good alternative, with good blood stability and no hERG affinity, providing new opportunities for the series. Overall, the obtained results suggest that further optimization of solubility and microsomal stability of the series could provide a strong lead for a new anti-TB drug development program.

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Reference:
Thiazole | C3H5001NS – PubChem,
Thiazole | chemical compound | Britannica

Extracurricular laboratory:new discovery of 4,5-Dimethylthiazol-2-amine

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One of the major hurdles in the development of safe and effective drugs targeting G-protein coupled receptors (GPCRs) is finding ligands that are highly selective for a specific receptor subtype. The search for novel compounds with therapeutic value by targeting the A3 adenosine receptor (A3AR) is still in its early stages. The increasing knowledge about the biological, physiological and pathological role of the A3AR subtype was accompanied by the design and development of the A3AR ligands, but the particular role of A3AR agonists and antagonists is still an open issue. Among the large variety of chemical classes screened towards ARs flavonoids have been indicated as remarkable A3AR antagonists. However, the search of A3AR ligands based on this framework seems to be discontinued. In this context, our research group focused its investigation into the discovery and development of novel, potent and selective AR ligands based on the chemical core of flavonoids, the chromone scaffold. The ongoing research has shown that chromone-2-phenylcarboxamide derivatives display a remarkable preference for hA3AR. In this work we report stimulating results, supported by A2A/A3 molecular docking simulations and structure-affinity-relationship (SAR) studies by which N-(4,5-methylthiazol-2-yl)-4-oxo-4H-chromene-2-carboxamide (compound 31) emerged as the most potent and selective compound, displaying an hA3Ki of 167 nM and a selectivity ratio of 590 vs. the hA1 and 480 vs. the hA2AAR subtypes. The chromone-based ligand was obtained by a simple synthetic approach and will enter in a lead optimization program to enhance its potency and drug-like properties.

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Reference:
Thiazole | C3H4993NS – PubChem,
Thiazole | chemical compound | Britannica

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One-pot syntheses of 5H-[1,3]thiazolo[2,3-b]quinazolin-5-one, 12H-[1,3]benzothiazolo[2,3-b]quinazolin-12-one, and corresponding derivatives were developed using the copper-catalyzed Ullmann condensation. The use of ultrasonic irradiation enhanced yields and reduced the reaction time to minutes. Copyright Taylor & Francis Group, LLC.

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Reference:
Thiazole | C3H4992NS – PubChem,
Thiazole | chemical compound | Britannica

Brief introduction of 4,5-Dimethylthiazol-2-amine

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2289-75-0, Name is 4,5-Dimethylthiazol-2-amine, molecular formula is C5H8N2S, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 2289-75-0, Recommanded Product: 2289-75-0

Compounds of the formula SPC1 Wherein R1 is hydrogen, methyl or ethyl, and Ar is phenyl, 3-chlorophenyl, 3-bromophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 3-tolyl, 2-methoxyphenyl, 3-methoxyphenyl, 2-pyridyl, 4-methyl-2-pyridyl, 6-methyl-2-pyridyl, 3-hydroxy-2-pyridyl, 3-pyridyl, 4-pyridyl, 6-chloro-3-pyridazinyl, 2-pyrazinyl, 6-chloro-2-pyrazinyl, 6-chloro-4-pyrimidinyl, 2-thiazolyl, 4-methyl-2-thiazolyl, 4-ethyl-2-thiazolyl, 5-methyl-2-thiazolyl, 5-ethyl-2-thiazolyl, 4,5-dimethyl-2-thiazolyl, 4-ethyl-5-methyl-2-thiazolyl, 5-ethyl-4-methyl-2-thiazolyl, 2-benzothiazolyl, 4,5,6,7-tetrahydro-2-benzothiazolyl, 5,6-dihydro-7H-thiopyrano[4,3-d]thiazol-2-yl, 3-methyl-5-isothiazolyl, 1,3,4-thiadiazolyl, 5-methyl-1,3,4-thiadiazol-2-yl or 5-methyl-3-isoxazolyl, And non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base; the compounds as well as their salts are useful as inhibitors of platelet adhesion and aggregation.

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Reference:
Thiazole | C3H5013NS – PubChem,
Thiazole | chemical compound | Britannica

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A series of thiazolidenebenzenesulfonamides have been discovered as nonnucleoside reverse transcriptase inhibitors. Compound 17a exhibited the most potent inhibitory activity against the Y181C mutant reverse transcriptase (RT). The introduction of the 4-chloro-5-isopropyl moiety (17k) markedly increased the activity against the wild type RT. Both 17a and 17k strongly inhibited HIV-1 replication. A random high-throughput screening (HTS) program to discover novel nonnucleoside reverse transcriptase inhibitors (NNRTIs) has been carried out with MT-4 cells against a nevirapine-resistant virus, HIV-1IIIB-R. The primary hit, a thiazolidenebenzenesulfonamide derivative, possessed good activity. A systematic modification program examining various substituents at the 3-, 4-, and 5-positions on the thiazole ring afforded compounds with enhanced anti-HIV-1 and reverse transcriptase (RT) inhibitory activities. These results confirm the important role of the substituents at these positions and the thiazolidenebenzenesulfonamide motif as a valuable lead series for the next generation NNRTIs.

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Reference:
Thiazole | C3H5024NS – PubChem,
Thiazole | chemical compound | Britannica

Simple exploration of 4,5-Dimethylthiazol-2-amine

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The invention relates to a process for the manufacture of 1:1 metal complexes of azines of the formula STR1 wherein R1 is a hydrogen atom, an alkyl or aryl group, R2 is an isocyclic or heterocyclic radical containing a hydroxyl or mercapto group adjacent to the azomethine group, Y is the radical of a compound which contains active methylene groups, or of an aryl or heteroaryl amine, and the ring A can contain substituents that do not confer solubility in water, which process comprises reacting a compound of the formula STR2 wherein R3 is a hydrogen atom or an alkyl radical, R4 is an alkyl, aryl or heteroaryl radical or the radical of the formula STR3 or R3 and R4, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, and Y has the given meaning, with a hydrazone of the formula STR4 in the presence of a transition metal donor and in a polar organic solvent, at temperatures above 100 C. Compared with pigments obtained by the prior art methods, the pigments of this invention have greater purity and better fastness properties, especially better fastness to migration, overspraying, light, atmospheric influences and heat.

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Reference:
Thiazole | C3H4971NS – PubChem,
Thiazole | chemical compound | Britannica