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
Letters in Drug Design & Discovery
Title: Antitubercular Properties of Substituted Hydroxycyclohexadienones
Volume: 3 Issue: 6
Author(s): Manish Shah, Geoffrey Wells, Tracey D. Bradshaw, Charles A. Laughton, Malcolm F.G. Stevens and Andrew D. Westwell
Affiliation:
Keywords: Antitubercular activity, Mycobacterium tuberculosis (MTb), quinols, thioredoxin
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.
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Cite this article as:
Shah Manish, Wells Geoffrey, Bradshaw D. Tracey, Laughton A. Charles, Stevens F.G. Malcolm and Westwell D. Andrew, Antitubercular Properties of Substituted Hydroxycyclohexadienones, Letters in Drug Design & Discovery 2006; 3 (6) . https://dx.doi.org/10.2174/157018006777805486
DOI https://dx.doi.org/10.2174/157018006777805486 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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