Azaindoles: Noncovalent DprE1 Inhibitors from Scaffold Morphing Efforts, Kill Mycobacterium tuberculosis and Are Efficacious in Vivo
2013
We report 1,4-azaindoles as a new inhibitor class that kills
Mycobacterium tuberculosisin vitro and demonstrates efficacy in mouse tuberculosis models. The series emerged from scaffold
morphingefforts and was demonstrated to noncovalently inhibit decaprenylphosphoryl-β-d-ribose2′-epimerase (DprE1). With “drug-like” properties and no expectation of
pre-existingresistance in the clinic, this chemical class has the potential to be developed as a therapy for drug-sensitive and drug-resistant tuberculosis.
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