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This review includes the non-patent literature up to October 2004 that deals with selective neuronal nitric oxide synthase inhibitors (highest potency is for the neuronal isozyme). Some non-selective inhibitors or selective inducible nitric oxide synthase inhibitors are mentioned if they are related to compounds that are discussed; structures of these compounds generally are not given. In vitro inhibition constants are given either as IC50 values or as Ki values. An IC50 value, the inhibitor concentration that produces 50% inhibition in the presence of a constant concentration of substrate, is obtained by extrapolation of several rate data points to 50% inhibition. Ki values are derived from several types of plots that relate the concentration of inhibitor with enzyme velocity in the presence of a variety of substrate concentrations [1]. The Ki value can be estimated from the IC50 value [2]. Although the two inhibition constants are related, they are not the same; generally, the reported Ki values tend to be lower than the IC50 values. If specifics are desired about how the data were collected, then the reader will have to look in the literature cited. No attempt was made to be exhaustive in citing all references related to specific inhibitors; rather, examples of literature references are given for each inhibitor described.

This review includes the non-patent literature up to October 2004 that deals with selective neuronal nitric oxide synthase inhibitors (highest potency is for the neuronal isozyme). Some non-selective inhibitors or selective inducible nitric oxide synthase inhibitors are mentioned if they are related to compounds that are discussed; structures of these compounds generally are not given. In vitro inhibition constants are given either as IC50 values or as Ki values. An IC50 value, the inhibitor concentration that produces 50% inhibition in the presence of a constant concentration of substrate, is obtained by extrapolation of several rate data points to 50% inhibition. Ki values are derived from several types of plots that relate the concentration of inhibitor with enzyme velocity in the presence of a variety of substrate concentrations [1]. The Ki value can be estimated from the IC50 value [2]. Although the two inhibition constants are related, they are not the same; generally, the reported Ki values tend to be lower than the IC50 values. If specifics are desired about how the data were collected, then the reader will have to look in the literature cited. No attempt was made to be exhaustive in citing all references related to specific inhibitors; rather, examples of literature references are given for each inhibitor described.

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Thiazole | C3H4949NS – PubChem,
Thiazole | chemical compound | Britannica

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The discovery and optimization of a novel series of FATP1 inhibitors are described. Through the derivatization process, arylpiperazine derivatives 5k and 12a were identified as possessing potent in vitro activity against human and mouse FATP1s as well as excellent pharmacokinetic properties. In vivo evaluation of triglyceride accumulation in the liver, white gastrocnemius muscle and soleus is also described.

The discovery and optimization of a novel series of FATP1 inhibitors are described. Through the derivatization process, arylpiperazine derivatives 5k and 12a were identified as possessing potent in vitro activity against human and mouse FATP1s as well as excellent pharmacokinetic properties. In vivo evaluation of triglyceride accumulation in the liver, white gastrocnemius muscle and soleus is also described.

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Thiazole | C3H4979NS – PubChem,
Thiazole | chemical compound | Britannica

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A series of 1,2-dihydro-1-oxopyrrolo<3,2,1-kl>phenothiazine, 1,2-dihydro-1-oxopyrrolo<3,2,1-kl>phenoxazine, and 1,2-dihydro-1-oxopyrrolo<3,2,1-de>acridine-2-carboxamides were prepared by reaction of 1,2-dihydro-1-oxopyrrolo<3,2,1-kl>phenothiazine or other corresponding phenoxazine and acridan ethyl or methyl esters with appropriate amines.Several members of this family were found to be potent, dual inhibitors of cyclooxygenase and 5-lipoxygenase pathways of arachidonic acid metabolism and to have in vivo antiinflammatory activity in the rat foot edema assay.Structure-activity relationships within this family of compounds are described. 1,2-Dihydro-N-(2-thiazolyl)-1-oxopyrrolo<3,2,1-kl>phenothiazine-1-carboxamide (34) was found to be one of the best compounds to display potent cyclooxygenase/5-lipoxygenase inhibition of arachidonic acid metabolism.Its IC50s against the enzymes sourced from rat basophillic leukemia-1 (RBL-1) cells were 0.07 and 1.4 muM, respectively.It was active in the rat foot edema test for antiinflammatory effect (48percent inhibition at 33 mg/kg po) and in the mouse phenylbenzoquinone induced writhing test for analgesic effect (93percent inhibition at 32 mg/kg po).

A series of 1,2-dihydro-1-oxopyrrolo<3,2,1-kl>phenothiazine, 1,2-dihydro-1-oxopyrrolo<3,2,1-kl>phenoxazine, and 1,2-dihydro-1-oxopyrrolo<3,2,1-de>acridine-2-carboxamides were prepared by reaction of 1,2-dihydro-1-oxopyrrolo<3,2,1-kl>phenothiazine or other corresponding phenoxazine and acridan ethyl or methyl esters with appropriate amines.Several members of this family were found to be potent, dual inhibitors of cyclooxygenase and 5-lipoxygenase pathways of arachidonic acid metabolism and to have in vivo antiinflammatory activity in the rat foot edema assay.Structure-activity relationships within this family of compounds are described. 1,2-Dihydro-N-(2-thiazolyl)-1-oxopyrrolo<3,2,1-kl>phenothiazine-1-carboxamide (34) was found to be one of the best compounds to display potent cyclooxygenase/5-lipoxygenase inhibition of arachidonic acid metabolism.Its IC50s against the enzymes sourced from rat basophillic leukemia-1 (RBL-1) cells were 0.07 and 1.4 muM, respectively.It was active in the rat foot edema test for antiinflammatory effect (48percent inhibition at 33 mg/kg po) and in the mouse phenylbenzoquinone induced writhing test for analgesic effect (93percent inhibition at 32 mg/kg po).

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Thiazole | C3H5032NS – PubChem,
Thiazole | chemical compound | Britannica

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The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

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Thiazole | C3H4961NS – PubChem,
Thiazole | chemical compound | Britannica

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The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 2289-75-0 is helpful to your research., Safety of 4,5-Dimethylthiazol-2-amine

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, Safety of 4,5-Dimethylthiazol-2-amine

Compounds of the formula STR1 wherein R1 is hydrogen, halogen or alkyl of 1 to 3 carbon atoms; R2 is hydrogen or alkyl of 1 to 3 carbon atoms; and R3 is aromatic hydrocarbyl of 6 to 10 carbon atoms or an aromatic heterocycle of 2 to 9 carbon atoms and 1 to 2 nitrogen atoms and/or an oxygen or a sulfur atom, where each of said aromatic substituents may in turn be substituted with one or two alkyls of 1 to 6 carbon atoms, halogen, hydroxyl, trifluoromethyl, halophenyl or alkoxy of 1 to 3 carbon atoms; and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases; the compounds as well as their salts are useful as analgesics, antipyretics, antithrombotic and antiphlogistics.

Compounds of the formula STR1 wherein R1 is hydrogen, halogen or alkyl of 1 to 3 carbon atoms; R2 is hydrogen or alkyl of 1 to 3 carbon atoms; and R3 is aromatic hydrocarbyl of 6 to 10 carbon atoms or an aromatic heterocycle of 2 to 9 carbon atoms and 1 to 2 nitrogen atoms and/or an oxygen or a sulfur atom, where each of said aromatic substituents may in turn be substituted with one or two alkyls of 1 to 6 carbon atoms, halogen, hydroxyl, trifluoromethyl, halophenyl or alkoxy of 1 to 3 carbon atoms; and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases; the compounds as well as their salts are useful as analgesics, antipyretics, antithrombotic and antiphlogistics.

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Reference£º
Thiazole | C3H5012NS – PubChem,
Thiazole | chemical compound | Britannica

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(Chemical Equation Presented) Condensation of 4-chloro-2-oxo-2H-chromene-3- carbonitrile (1) with heteroarylamines 2a-d in acetonitrile containing a catalytic amount of triethylamine followed by spontaneous intramolecular cyclization gave the novel coumarin derivatives 3a-d, respectively. These compounds underwent acid hydrolysis giving the corresponding oxoderivatives 4a-d. The structural assignments of the synthesized compounds were based on elemental, IR, 1H and 13C NMR analyses.

(Chemical Equation Presented) Condensation of 4-chloro-2-oxo-2H-chromene-3- carbonitrile (1) with heteroarylamines 2a-d in acetonitrile containing a catalytic amount of triethylamine followed by spontaneous intramolecular cyclization gave the novel coumarin derivatives 3a-d, respectively. These compounds underwent acid hydrolysis giving the corresponding oxoderivatives 4a-d. The structural assignments of the synthesized compounds were based on elemental, IR, 1H and 13C NMR analyses.

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Thiazole | C3H5046NS – PubChem,
Thiazole | chemical compound | Britannica

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The corrosion behavior of iron in diluted aqueous sulfuric acid medium has been studied in the presence and absence of 6-ethoxybenzo[d]thiazol-2-amine (EBT), 5-bromothiazol-2-amine (BTA) and 4,5-dimethylthiazol-2-amine (DTA). Potentiodynamic measurements showed the shift of corrosion potential towards a more negative potential indicating that these compounds mostly act as cathodic inhibitors due to their adsorption on the iron surface. The adsorbed film of these molecules hinders the transport of metal ions from the metal to the solution and also retards hydrogen evolution reaction by acting as a physical barrier. The molecules were also studied by density functional theory (DFT), using the B3LYP functional in order to determine the relationship between molecular structure and the corrosion inhibition efficiencies.

The corrosion behavior of iron in diluted aqueous sulfuric acid medium has been studied in the presence and absence of 6-ethoxybenzo[d]thiazol-2-amine (EBT), 5-bromothiazol-2-amine (BTA) and 4,5-dimethylthiazol-2-amine (DTA). Potentiodynamic measurements showed the shift of corrosion potential towards a more negative potential indicating that these compounds mostly act as cathodic inhibitors due to their adsorption on the iron surface. The adsorbed film of these molecules hinders the transport of metal ions from the metal to the solution and also retards hydrogen evolution reaction by acting as a physical barrier. The molecules were also studied by density functional theory (DFT), using the B3LYP functional in order to determine the relationship between molecular structure and the corrosion inhibition efficiencies.

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Thiazole | C3H4980NS – PubChem,
Thiazole | chemical compound | Britannica

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Free fatty acid receptor 2 (FFA2) is a G-protein coupled receptor for which only short-chain fatty acids (SCFAs) have been reported as endogenous ligands. We describe the discovery and optimization of phenylacetamides as allosteric agonists of FFA2. These novel ligands can suppress adipocyte lipolysis in vitro and reduce plasma FFA levels in vivo, suggesting that these allosteric modulators can serve as pharmacological tools for exploring the potential function of FFA2 in various disease conditions.

Free fatty acid receptor 2 (FFA2) is a G-protein coupled receptor for which only short-chain fatty acids (SCFAs) have been reported as endogenous ligands. We describe the discovery and optimization of phenylacetamides as allosteric agonists of FFA2. These novel ligands can suppress adipocyte lipolysis in vitro and reduce plasma FFA levels in vivo, suggesting that these allosteric modulators can serve as pharmacological tools for exploring the potential function of FFA2 in various disease conditions.

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Thiazole | C3H5007NS – PubChem,
Thiazole | chemical compound | Britannica

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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2289-75-0,4,5-Dimethylthiazol-2-amine,as a common compound, the synthetic route is as follows.

e. N-(4,5-Dimethyl-2-thiazolyl)-4-hydroxy-2-methyl-2H-naphtho[2,1-e]-1,2-thiazine-3-carboxamide-1,1-dioxide, m.p. 264-265 C (decomp., from ethylene chloride), from 2-methyl-4-(1-pyrrolidyl)-2-H-naphtho[2,1-e]-1,2-thiazine-3-carboxylic acid chloride-1,1-dioxide and 2-amino-4,5-dimethyl-thiazole.

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Reference£º
Patent; Boehringer Ingelheim GmbH; US3992535; (1976); A;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

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2289-75-0, 4,5-Dimethylthiazol-2-amine is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1N-(4,5-dimethylthiazol-2-yl)-2-[5-(6,7-dimethoxyquinazolin-4-yloxy)pyridin-2- yl]acetamideTriethylamine (0.245 ml) and 2-(7-azabenzotriazol-l-yl)-l,l,3,3-tetramethyluronium hexafluoropliosphate(V) (0.236 g) were added in turn to a stirred mixture of2-[5-(6,7-dimethoxyquinazolin-4-yloxy)pyridin-2-yl]acetic acid (0.2 g), 2-amino- 4,5-dimethylthiazole (0.083 g) and DMF (2 ml) and the resultant mixture was stirred at ambient temperature for 40 minutes. A mixture of a saturated aqueous sodium bicarbonate solution (5 ml) and a saturated aqueous sodium carbonate solution (5 ml) was added and the resultant mixture was stirred at ambient temperature for 1 hour. The precipitate was isolated and triturated under diethyl ether. The resultant solid was dried under vacuum at 400C for 16 hours. There was thus obtained the title compound as a solid (0.185 g); 1H NMR: (DMSOd6) 2.1 (s, 3H), 2.2 (s, 3H), 4.0 (m, 8H), 7.4 (s, IH), 7.5 (d, IH), 7.6 (s, IH), 7.8 (m, IH), 8.5 (m, IH), 8.55 (s, IH): Mass Spectrum: M-H’ 450., 2289-75-0

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Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/99317; (2007); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica