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Synthesis and Evaluation of Potent Ene–yne Inhibitors of Type II Dehydroquinases as Tuberculosis Drug Leads
Author(s) -
Tran Anh Thu,
Cergol Katie M.,
West Nicholas P.,
Randall Elizabeth J.,
Britton Warwick J.,
Bokhari Syed Ali Imran,
Ibrahim Musadiq,
Lapthorn Adrian J.,
Payne Richard J.
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000399
Subject(s) - mycobacterium tuberculosis , tuberculosis , streptomyces coelicolor , shikimate pathway , in vitro , drug , chemistry , biology , pharmacology , stereochemistry , streptomyces , medicine , bacteria , biochemistry , gene , biosynthesis , genetics , pathology
E‐9: You sunk my battleship! Potent ene–yne‐based inhibitors of type II dehydroquinase are described. The majority of the compounds exhibited nanomolar inhibition of the Streptomyces coelicolor, Helicobacter pylori and Mycobacterium tuberculosis type II dehydroquinases. The inhibitors also possessed moderate activity against the growth of M. tuberculosis in vitro.