Synthesis of N-substituted indole derivatives as potential antimicrobial and antileishmanial agents.

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ID: 104536
2020
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Abstract
Leishmaniasis and microbial infections are two of the major contributors to global mortality and morbidity rates. Hence, development of novel, effective and safer antileishmanial and antimicrobial agents having reduced side effects are major priority for researchers. Two series of N-substituted indole derivatives i.e. N-substituted indole based chalcones (12a-g) and N-substituted indole based hydrazide-hydrazones (18a-g, 19a-f, 21 a-g) were synthesized. The synthesized compounds were characterized by H NMR, C NMR, Mass and FT-IR spectral data. Further these derivatives were evaluated for their antimicrobial potential against Escherichia coli, Bacillus subtilis, Pseudomonas putida and Candida viswanathii, and antileishmanial potential against promastigotes of Leishmania donovani. Compounds 18b, 18d and 19d exhibited significant activity with an IC of 0.19 ± 0.03 µM, 0.14 ± 0.02 µM and 0.16 ± 0.06 µM against B. subtilis which was comparable to chloramphenicol (IC of 0.25 ± 0.03 µM). Compounds 12b and 12c exhibited an IC of 24.2 ± 3.5 µM and 21.5 ± 2.1 µM in the antileishmanial assay. Binding interactions of indole based hydrazide-hydrazones were studied with nitric oxide synthase in silico in order to understand the structural features responsible for activity.
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tiwari2020synthesisbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Tiwari, Shweta;Kirar, Seema;Banerjee, Uttam Chand;Neerupudi, Kishore Babu;Singh, Sushma;Wani, Aabid Abdullah;Bharatam, Prasad V;Singh, Inder Pal;
Journal Bioorganic chemistry
Year 2020
DOI
S0045-2068(19)32126-1
URL
Keywords
Antimicrobial activity chalcones indole hydrazide-hydrazones antileishmanial activity

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