4.2 Article

Synthesis, characterization, docking study and antimicrobial activity of 2-(4-benzoylphenoxy)-1-[2-(1-methyl-1H-indol-3-yl)methyl)-1H-benzo[d]imidazol-1-yl] ethanone derivatives

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JOURNAL OF THE IRANIAN CHEMICAL SOCIETY
卷 18, 期 10, 页码 2741-2756

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DOI: 10.1007/s13738-021-02230-y

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  1. UGC New Delhi [F.39-737/2010 (SR)]

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The study focuses on the development of new antibacterial agents with different mechanisms of action from traditional antibiotics, showing potential for combating drug-resistant bacterial infections. By synthesizing new benzimidazole bridged benzophenone substituted indole scaffolds, potent compounds were identified, with FtsZ protein recognized as a potential target. Docking studies confirmed the in vitro findings, highlighting compounds 11b, 11e, 11f, and 11h as effective molecules in the series.
The occurrence of drug-resistant bacterial infections impulses the development of new antibacterial agents that own a mechanism of action different from traditional antibiotics. From the earlier days, benzophenone, indole and benzimidazole moieties alone are one of the most important frameworks in the discovery of innovative drugs. In this present study, we have described a detailed synthesis and structural elucidation of new benzimidazole bridged benzophenone substituted indole scaffolds 11a-k. Further, all the newly synthesized compounds were tested for in vitro antimicrobial activity by disk diffusion and serial dilution method and the compounds 11b, 11e, 11f and 11h were revealed as potent compounds among the tested strains in the series11a-k. Further, compounds 11b, 11e, 11f and 11h were subjected for in silico studies and FtsZ has been recognized as a key functional protein in bacterial cell division and it is currently considered to be a potential target for the growth of novel antibacterial agents. In continuation, the results obtained from docking studies were in accordance with in vitro results and compounds 11b, 11e, 11f and 11h emerged as potent molecules in the series 11a-k.

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