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Design and synthesis of triazolopyrimidine acylsulfonamides as novel anti-mycobacterial leads acting through inhibition of acetohydroxyacid synthase.

Abstract：

:Novel triazolopyrimidine acylsulfonamides class of antimycobacterial agents, which are mycobacterial acetohydroxyacid synthase (AHAS) inhibitors were designed by hybridization of known AHAS inhibitors such as sulfonyl urea and triazolopyrimidine sulfonamides. This Letter describes the synthesis and SAR studies of this class of molecules by variation of two parts of the molecule, the phenyl and triazolopyrimidine rings. SAR study describes optimisation of enzyme potency, whole cell potency and evidence of mechanism of action.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Patil V,Kale M,Raichurkar A,Bhaskar B,Prahlad D,Balganesh M,Nandan S,Shahul Hameed P

doi

10.1016/j.bmcl.2014.02.054

subject

Has Abstract

pub_date

2014-05-01 00:00:00

pages

2222-5

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00186-3

journal_volume

24

pub_type

杂志文章

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