9/23 News New explortion of Ethyl 1,3-benzothiazole-2-carboxylate

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The strong therapeutic potential of CB2 receptor agonists for use as anti-inflammatory agents that lack psychiatric side effects has attracted substantial interest. We herein describe the rational design and synthesis of novel thiazole and benzothiazole derivatives and the evaluation of their binding affinity and functional activity on CB1 and CB2 receptors. The series with the general formula N-(3-pentylbenzo [d]thiazol-2(3H)-ylidene) carboxamide (compounds 6a-6d) exhibited the highest affinity and selectivity towards CB2 receptors with Kis in the picomolar or low nanomolar range, and selectivity indices (Ki hCB1/Ki hCB2) reaching up to 429 fold. Notably, these compounds also demonstrated an agonistic functional activity in cellular assays with EC50s in the low nanomolar range. More interestingly, compound 6d, the 3-(trifluoromethyl)benzamide derivative, exhibited remarkable protection against DSS-induced acute colitis in mice model.

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Reference:
Thiazole | C3H7681NS – PubChem,
Thiazole | chemical compound | Britannica

Sep 2021 News Awesome Chemistry Experiments For Ethyl 1,3-benzothiazole-2-carboxylate

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2-Acetoacetylbenzothiazole (III) has been prepared either by the reaction between ethyl benzothiazole-2-carboxylate (I) and acetone or by the reaction of 2-benzothiazolyl methyl ketone (II) with ethyl acetate.Condensation of III with hydrazines affords the title componds (V) through the intermediacy of hydrazone (IV).The mass spectra of V reveal that the molecular ion undergoes fragmentation via three principal modes: (a) fission of benzothiazole ring, (b) fission of pyrazole ring resulting either in the loss of N2R radical or in the formation of aryldiazonium cation,and (c) fission of pyrazole ring with concomitant loss of CH3CN.Compound IVc (R = 0C6H5) exhibits mild antiinflammatory activity.

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Reference:
Thiazole | C3H7720NS – PubChem,
Thiazole | chemical compound | Britannica

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 32137-76-1, Name is Ethyl 1,3-benzothiazole-2-carboxylate, molecular formula is C10H9NO2S. In a Article,once mentioned of 32137-76-1, COA of Formula: C10H9NO2S

The reactions of ethyl carboethoxyformimidate with various bidentate reagents illustrate its usefulness as a reagent in heterocyclic chemistry.

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Reference:
Thiazole | C3H7682NS – PubChem,
Thiazole | chemical compound | Britannica

Final Thoughts on Chemistry for Ethyl 1,3-benzothiazole-2-carboxylate

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It is proposed that the reported condensation between 2-aminobenzenethiol and diethyloxalate give rise to 2-ethoxycarbonylbenzothiazole 3 rather than 3-ethoxy-2H-1,4-benzothiazin-2-one 2.

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Reference:
Thiazole | C3H7698NS – PubChem,
Thiazole | chemical compound | Britannica

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The aza-Wittig reaction of 2-methylthio-N-triphenylphosphoranylideneaniline (2) with acid chlorides (3) in refluxing benzene or toluene afforded 2-substituted 1,3-benzothiazoles (6).

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Reference:
Thiazole | C3H7694NS – PubChem,
Thiazole | chemical compound | Britannica

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Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.

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Thiazole | C3H7704NS – PubChem,
Thiazole | chemical compound | Britannica

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We present the first base-free Fe-catalyzed ester reduction applying molecular hydrogen. Without any additives, a variety of carboxylic acid esters and lactones were hydrogenated with high efficiency. Computations reveal an outer-sphere mechanism involving simultaneous hydrogen transfer from the iron center and the ligand. This assumption is supported by NMR experiments.

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Thiazole | C3H7674NS – PubChem,
Thiazole | chemical compound | Britannica

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Various aromatic bromides were treated with n-BuLi and subsequently with ethyl formate, followed by the reaction with ethanol and molecular iodine in the presence of K2CO3 to provide the corresponding aromatic ethyl esters in good yields. Moreover, aromatic bromides could be transformed into the corresponding aromatic methyl esters in good yields by the treatment with n-BuLi and subsequently with DMF, followed by the reaction with methanol, molecular iodine, and K2CO3. Some aromatics could be also converted into the corresponding aromatic esters in good yields by the treatment with n-BuLi, and subsequently with ethyl formate or DMF, followed by the reaction with molecular iodine and K2CO3. The present reactions offer a novel route for the transition-metal-free, carbon-monoxide-free, and therefore environmentally benign one-pot conversion of aromatic bromides and aromatics into aromatic esters.

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Thiazole | C3H7675NS – PubChem,
Thiazole | chemical compound | Britannica

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Abstract: A new series of benzothiazole amide derivatives (9a?l) were synthesized and characterized by Fourier-transform infrared (FT-IR), mass, and 1H and 13C nuclear magnetic resonance (NMR) spectroscopic techniques. The antimitotic activity of the newly synthesized compounds was determined by the Allium assay method, from which mitotic index values were calculated. Here, 9g (14.0 %) and 9l (14.5 %) showed mitotic index values most comparable to that of standard drug (14.4 %), while the remaining compounds showed lower mitotic index values; hence, these compounds inhibit the regular cell division process and are the most promising antimitotic agents. Based on the structural activity relationship, the maximum percentage inhibition was observed for compounds containing electron-withdrawing group, revealing enhanced antimitotic activity, while compounds with electron-donating groups such as furan (9g) and methyl (9l) were comparable to standard. The newly synthesized compounds were also screened for antimicrobial activity, with some of them showing remarkable activity. Graphical Abstract: [Figure not available: see fulltext.]

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Reference:
Thiazole | C3H7711NS – PubChem,
Thiazole | chemical compound | Britannica

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Quinuclidine-substituted hetero-bicyclic aromatic compounds for the treatment of disease

The invention provides compounds of Formula I: 1wherein W0 is a bicyclic moiety and is 2These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful to treat diseases or conditions in which alpha7 is known to be involved.

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Reference:
Thiazole | C3H7688NS – PubChem,
Thiazole | chemical compound | Britannica