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Indole chalcones: Design, synthesis, in vitro and in silico evaluation against Mycobacterium tuberculosis.

Abstract：

:Indole chalcones were designed and synthesized as a promising set of compounds against H37Rv strain of Mycobacterium tuberculosis. Within this library of compounds, (E)-1-(furan-3-yl)-3-(1H-indol-3-yl)prop-2-en-1-one (18), (E)-3-(1H-indol-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one (20) and (E)-2-((1H-indol-2-yl)methylene)cyclopentan-1-one (24) displayed high anti-tubercular activity at 50 μg/ml with MIC values of 210, 197 and 236 μM respectively. The in-silico studies revealed that compound 18 exhibit binding modes similar to FAS-II inhibitors like INH or Thiolactomycin against KasA protein. Cytotoxicity assay results suggest that the compounds 18, 20 and 24 are non-cytotoxic to human megakaryocytes and murine B cells.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Ramesh D,Joji A,Vijayakumar BG,Sethumadhavan A,Mani M,Kannan T

doi

10.1016/j.ejmech.2020.112358

subject

Has Abstract

pub_date

2020-07-15 00:00:00

pages

112358

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(20)30328-7

journal_volume

198

pub_type

杂志文章

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