Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Antitubercular Properties of Substituted Hydroxycyclohexadienones

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

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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Article Details

VOLUME: 3
ISSUE: 6
Year: 2006
Page: [419 - 423]
Pages: 5
DOI: 10.2174/157018006777805486
Price: $58