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.

ABSTRACT: 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 μM. 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<

SUBMITTER: Srinivasarao S 

PROVIDER: S-EPMC9050811 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature