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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Antitubercular Properties of Substituted Hydroxycyclohexadienones

Author(s): Manish Shah, Geoffrey Wells, Tracey D. Bradshaw, Charles A. Laughton, Malcolm F.G. Stevens and Andrew D. Westwell

Volume 3, Issue 6, 2006

Page: [419 - 423] Pages: 5

DOI: 10.2174/157018006777805486

Price: $65

Abstract

The in vitro evaluation of a series of (hetero)aromatic-substituted 4-hydroxycyclohexa-2,5-dienones (quinols) and analogues against M. tuberculosis is reported. The most active compound in the series was found to be 4-(benzothiazol-2-yl)-4-hydroxycyclohexa-2,5-dienone 1a with a minimum inhibitory concentration of 0.78 μg/mL. Biochemical evidence for involvement of the small redox protein thioredoxin C - a novel drug target - is also presented.

Keywords: Antitubercular activity, Mycobacterium tuberculosis (MTb), quinols, thioredoxin


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