Antitubercular Properties of Substituted Hydroxycyclohexadienones
Tracey D. Bradshaw,
Charles A. Laughton,
Malcolm F.G. Stevens,
Andrew D. Westwell.
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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