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2-Aryl benzazole derived new class of anti-tubercular compounds: Endowed to eradicate mycobacterium tuberculosis in replicating and non-replicating forms.

Abstract：

:The high mortality rate and the increasing prevalence of Mtb resistance are the major concerns for the Tuberculosis (TB) treatment in this century. To counteract the prevalence of Mtb resistance, we have synthesized 2-aryl benzazole based dual targeted molecules. Compound 9m and 9n were found to be equally active against replicating and non-replicating form of Mtb (MIC(MABA) 1.98 and 1.66 μg/ml; MIC(LORA) 2.06 and 1.59 μg/ml respectively). They arrested the cell division (replicating Mtb) by inhibiting the GTPase activity of FtsZ with IC50 values 45 and 64 μM respectively. They were also capable of kill Mtb in non-replicating form by inhibiting the biosynthesis of menaquinone which was substantiated by the MenG inhibition (IC50 = 11.62 and 7.49 μM respectively) followed by the Vit-K2 rescue study and ATP production assay.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Velappan AB,Datta D,Ma R,Rana S,Ghosh KS,Hari N,Franzblau SG,Debnath J

doi

10.1016/j.bioorg.2020.104170

subject

Has Abstract

pub_date

2020-10-01 00:00:00

pages

104170

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(20)31467-X

journal_volume

103

pub_type

杂志文章

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