An article Seeking potent anti-tubercular agents: design and synthesis of substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives as anti-tubercular agents WOS:000526839700017 published article about MYCOBACTERIUM-TUBERCULOSIS; ANTIMYCOBACTERIAL EVALUATION; IN-VITRO; DOCKING; ANALOGS in [Srinivasarao, Singireddi; Nandikolla, Adinarayana; Suresh, Amaroju; Aggarwal, Himanshu; Sekhar, Kondapalli Venkata Gowri Chandra] Birla Inst Technol & Sci, Dept Chem, Hyderabad Campus, Hyderabad 500078, Telangana, India; [Calster, Kevin Van; De Voogt, Linda; Cappoen, Davie] Univ Ghent, Fac Biosci Engn, Dept Green Chem & Technol, Coupure Links 653, B-9000 Ghent, Belgium; [Ghosh, Balaram] Birla Inst Technol & Sci, Dept Pharm, Hyderabad Campus, Hyderabad 500078, Telangana, India; [Murugesan, Sankaranarayanan] Birla Inst Technol & Sci, Dept Pharm, Med Chem Res Lab, Pilani 333031, Rajasthan, India in 2020, Cited 34. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Recommanded Product: 98-97-5
Pyrazinamide is an important first-line drug used in shortening TB therapy. In our current work, a series of novel substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives were designed, synthesized, and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra. Among the tested compounds, five compounds (6a, 6e, 6h, 6j and 6k) from Series-I and one compound (7e) from Series-II exhibited significant activity against Mycobacterium tuberculosis H37Ra with 50% inhibitory concentrations (IC50) ranging from 1.35 to 2.18 mu M. To evaluate the efficacy of these compounds, we examined their IC90 values. Five of the most active compounds were found to be more active with IC(90)s ranging from 3.73 to 4.00 mu M and one compound (6e) showed an IC90 of 40.32 mu M. Moreover, single crystals were developed for 6d, 6f and 6n. In addition, most active compounds were evaluated for their cytotoxicity on HEK-293 (human embryonic kidney) cells. Our results indicate that the compounds are nontoxic to human cells. The molecular interactions of the derivatised conjugates in docking studies reveal their suitability for further development.
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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem