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Design, synthesis and evaluation of new thiadiazole- based direct inhibitors of enoyl acyl carrier protein reductase (InhA) for the treatment of tuberculosis
Šink, Roman ...
Mycobacterial enoyl acyl carrier protein reductase (InhA) is a clinically validated target for the treatment of tuberculosis infections, a disease that still causes the death of at least a million ...people annually. A known class of potent, direct and competitive InhA inhibitors based on a tetracyclic thiadiazole structure has been shown to have in-vivo activity in murine models of tuberculosis infection. Based on this template, we have here explored the medicinal chemistry of truncated analogues that have only three aromatic rings. In particular, compounds 8b, 8d, 8f, 8l and 8n show interesting features, including low nanomolar InhA IC50, sub-micromolar antimycobacterial potency, and improved physicochemical profiles in comparison with the tetracyclic analogues. From this series, 8d is identified as having the best balance of potency and properties, whereby the resolved 8d S-enatiomer shows encouraging in-vivo efficacy.
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