9/22/21 News More research is needed about 2-Mercaptobenzo[d]thiazole-6-carbonitrile

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The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R> R2, R6, and R7 are defined herein

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Reference:
Thiazole | C3H3559NS – PubChem,
Thiazole | chemical compound | Britannica

9/22/21 News Some scientific research about 2-Thiazolecarboxaldehyde

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A new tripodal ligand, tris[2-(((2-thiazolyl)methylidene)amino)ethyl]amine (Tatren), has been synthesized and characterized by NMR, IR, and UV-visible absorbance spectroscopy and elemental analysis. Tatren forms stable complexes with transition metal ions (Zn2+, 1; Mn2+, 2; Co 2+, 3) and the alkaline earth metal ions (Ca2+, 4; Mg 2+, 5). Single-crystal X-ray structures of 1, 2, and 5 revealed six-coordinate chelate complexes with formula [M(Tatren)]-(ClO4) 2 in which the metal centers are coordinated by three thiazolyl N atoms and three acyclic imine N atoms. Crystals of 1, 2, and 5 are monoclinic, P21/c space group. Crystals of 4 are triclinic, P1 space group. The Ca 2+ complex is eight-coordinate with all N atoms of Tatren and one water molecule coordinated to the metal ion. Spectrophotometric titrations show that formation constants for the chelates of metal ions are ?1 in methanol. Free Tatren inhibits the catalytic domain of matrix metalloproteinase-13 (MMP-13, collagenase-3) with Ki = 3.5 ± 0.6 muM. Molecular mechanics-based docking calculations suggest that one leg of Tatren coordinates to the catalytic Zn2+ in MMPs-2, -9, and -13 with significant hydrogen bonding to backbone amide groups. High-level DFT calculations suggest that, in the absence of nonbonded interactions between Tatren and the enzyme, the most stable first coordination sphere of the catalytic Zn2+ is achieved with three imidazolyl groups from His residues and two imine N atoms from one leg of Tatren. While complexes (1-3) do not inhibit MMP-13 to a significant extent, 4 does (Ki = 30 ± 10 muM). Hence, this study shows that tripodal chelating ligands of this class and their Ca 2+ complexes have potential as active-site inhibitors for MMPs.

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Reference:
Thiazole | C3H4474NS – PubChem,
Thiazole | chemical compound | Britannica

9/22 News Brief introduction of 4,5-Dimethylthiazol-2-amine hydrochloride

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The present invention relates to agents for coloring keratin fibers which comprise at least one cationic azodye of the general formula (I).

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Reference:
Thiazole | C3H5052NS – PubChem,
Thiazole | chemical compound | Britannica

22-Sep-21 News Archives for Chemistry Experiments of 5-Bromobenzothiazole

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A mild, copper-catalyzed coupling of organoindium reagents with nitrogen-containing aromatic heterocycles and chloroformates is described. This reaction proceeds with a range of organoindium reagents, yielding predominately or exclusively the 1,4-addition products with pyridine. In addition, a range of other nitrogen-containing heterocycles can be employed in this reaction (e.g. benzoxazole, benzothiazole, phthalazine). As an illustration of the utility of this reaction, this heterocycle functionalization is coupled with a subsequent oxidation to achieve the one-pot synthesis of functionalized pyridine and benzothiazole derivatives.

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Reference:
Thiazole | C3H6154NS – PubChem,
Thiazole | chemical compound | Britannica

22-Sep News Final Thoughts on Chemistry for Ethyl 2-(trifluoromethyl)thiazole-4-carboxylate

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133046-46-5, Name is Ethyl 2-(trifluoromethyl)thiazole-4-carboxylate, molecular formula is C7H6F3NO2S, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 133046-46-5, Safety of Ethyl 2-(trifluoromethyl)thiazole-4-carboxylate

Transition metal?catalyzed arene functionalization has been widely used for molecular synthesis over the past century. In this arena, copper catalysis has long been considered a privileged platform due to the propensity of high-valent copper to undergo reductive elimination with a wide variety of coupling fragments. However, the sluggish nature of oxidative addition has limited copper?s capacity to broadly facilitate haloarene coupling protocols. Here, we demonstrate that this copper oxidative addition problem can be overcome with an aryl radical?capture mechanism, wherein the aryl radical is generated through a silyl radical halogen abstraction. This strategy was applied to a general trifluoromethylation of aryl bromides through dual copper-photoredox catalysis. Mechanistic studies support the formation of an open-shell aryl species.

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Reference:
Thiazole | C3H7887NS – PubChem,
Thiazole | chemical compound | Britannica

9/22/21 News Awesome and Easy Science Experiments about 4-Methylthiazol-2-amine

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Related Products of 1603-91-4, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 1603-91-4, Name is 4-Methylthiazol-2-amine, molecular formula is C4H6N2S. In a Article,once mentioned of 1603-91-4

Mast cell derived leukotrienes (LT’s) play a vital role in pathophysiology of allergy and asthma. We synthesized various analogues of indolyl, naphthyl and phenylethyl substituted halopyridyl, thiazolyl and benzothiazolyl thioureas and examined their in vitro effects on the high affinity IgE receptor/FcepsilonRI-mediated mast cell leukotriene release. Of the 22 naphthylethyl thiourea compounds tested, there were 7 active compounds and N-[1-(1-naphthyl)ethyl]-N?-[2-(ethyl-4-acetylthiazolyl)]thiourea (17 and 16) (IC50=0.002 muM) and N-[1-(1R)-naphthylethyl]-N?-[2-(5-methylpyridyl)]thiourea (compound 5) (IC50=0.005 muM) were identified as the lead compounds. Among the 11 indolylethyl thiourea compounds tested, there were seven active compounds and the halopyridyl compounds N-[2-(3-indolylethyl)]-N?-[2-(5-chloropyridyl)]thiourea (24) and N-[2-(3-indolylethyl)]-N?-[2-(5-bromopyridyl)]thiourea (25) were the most active agents and inhibited the LTC4 release with low micromolar IC50 values of 4.9 and 6.1 muM, respectively. The hydroxylphenyl substituted compounds N-[2-(4-hydroxyphenyl)ethyl]-N?-[2-(5-chloropyridyl)]thiourea (37; IC50=12.6 muM), N-[2-(4-hydroxyphenyl)ethyl]-N?-[2-(5-bromopyridyl)]thiourea (50; IC50=16.8 muM) and N-[2-(4-hydroxyphenyl)ethyl]-N?-[2-(pyridyl)]thiourea (35; IC50=8.5 muM) were the most active pyridyl thiourea agents. Notably, the introduction of electron withdrawing or donating groups had a marked impact on the biological activity of these thiourea derivatives and the Hammett sigma values of their substituents were identified as predictors of their potency. In contrast, experimentally determined partition coefficient values did not correlate with the biological activity of the thiourea compounds which demonstrates that their liphophilicity is not an important factor controlling their mast cell inhibitory effects. These results establish the substituted halopyridyl, indolyl and naphthyl thiourea compounds as a new chemical class of anti-allergic agents inhibiting IgE receptor/FcepsilonRI-mediated mast cell LTC4 release. Further lead optimization efforts may provide the basis for new and effective treatment as well as prevention programs for allergic asthma in clinical settings.

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Reference:
Thiazole | C3H9768NS – PubChem,
Thiazole | chemical compound | Britannica

Sep-21 News Extended knowledge of 2-Thiazolecarboxaldehyde

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10200-59-6, Name is 2-Thiazolecarboxaldehyde, molecular formula is C4H3NOS, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 10200-59-6, Safety of 2-Thiazolecarboxaldehyde

The synthesis of a new heterocyclic benzimidazolo-pyridazinones is described.The new compounds were evaluated as inotropic agents with ‘calcium-sensitizing’ effects. 5-Methyl-6-<2-(3-pyrazolyl)-5-benzimidazolyl>-2,3,4,5-tetrahydro-pyridazin-3-one hydrochloride (meribendan) turned out to be the most interesting compound and was chosen for development as a positive inotrope. benzimidazole / calcium sensivity / cardiotonics / inotropes / phosphodiesterase / papillary muscle / pyridazinone

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Reference:
Thiazole | C3H4123NS – PubChem,
Thiazole | chemical compound | Britannica

22-Sep-21 News A new application about 5-Methylbenzo[d]thiazole-2-thiol

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(Chemical Equation Presented) The development of high-load, oligomeric benzylsulfonium salts, generated via ring-opening metathesis polymerization, and their utility in facile benzylations of various nucleophiles is reported. These oligomeric sulfonium salts exist as free-flowing powders and are stable at room temperature. After the benzylation event, purification is attained via simple dry load/filtration, followed by solvent removal to deliver products in excellent yield and purity.

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Reference:
Thiazole | C3H6489NS – PubChem,
Thiazole | chemical compound | Britannica

22-Sep News The important role of 2-Bromobenzothiazole

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Disclosed are compounds of Formula (I) to (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII); or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a bicyclic heteroaryl group substituted with zero to 3 R3a; and R1, R2, R3a, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.

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Reference:
Thiazole | C3H2718NS – PubChem,
Thiazole | chemical compound | Britannica

22-Sep-21 News New explortion of 4-(4-Chlorophenyl)thiazol-2-amine

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A total of thirty five new N-[4-(1,3-benzothiazol-2-yl)phenyl]acetamide derivatives were synthesized and structures of all the compounds were confirmed on the basis of elemental analysis and collective use of IR, 1H NMR, 13C NMR and mass spectral data. Compounds were tested for their ability to inhibit human monoacylglycerol lipase (hMAGL) enzyme. Eight compounds 4, 19-21, 24-26, and 34 reduced the hMAGL activity less than 50% at 100 nM concentrations. The halogen substituted aniline derivatives 20, 21 and 24-26 were found to be most active among all the synthesized compounds having IC50 value in the range of 6.5-9 nM. Twenty five compounds were selected by NCI, USA for one dose anticancer screening. Compound 21 (NSC: 780167) and 24 (NSC: 780168) fulfilled prearranged doorstep growth inhibition criteria and further selected for NCI full panel five dose assay at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 muM). Both the compounds 21 and 24 were found to be most active against MCF7 and MDA-MB-468 breast cancer cell lines. The GI50 value of 32.5 nM (MCF7) and 23.8 nM (MDA-MB-468) was observed for compound 21. Compound 24 showed GI50 values of 37.1 nM against MCF7 breast cancer cell line and 25.1 nM against MDA-MB-468 breast cancer cell line.

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Reference:
Thiazole | C3H10260NS – PubChem,
Thiazole | chemical compound | Britannica