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Identification of a novel class of quinoline-oxadiazole hybrids as anti-tuberculosis agents.

Abstract：

:A series of novel quinoline-oxadiazole hybrid compounds was designed based on stepwise rational modification of the lead molecules reported previously, in order to enhance bioactivity and improve druglikeness. The hybrid compounds synthesized were screened for biological activity against Mycobacterium tuberculosis H37Rv and for cytotoxicity in HepG2 cell line. Several of the hits exhibited good to excellent anti-tuberculosis activity and selectivity, especially compounds 12m, 12o and 12p, showed minimum inhibitory concentration values<0.5μM and selectivity index>500. The results of this study open up a promising avenue that may lead to the discovery of a new class of anti-tuberculosis agents.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Jain PP,Degani MS,Raju A,Anantram A,Seervi M,Sathaye S,Ray M,Rajan MGR

doi

10.1016/j.bmcl.2015.11.057

subject

Has Abstract

pub_date

2016-01-15 00:00:00

pages

645-649

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)30265-1

journal_volume

26

pub_type

杂志文章

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