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J Med Chem. 2013 Dec 12;56(23):9701-8. doi: 10.1021/jm401382v. Epub 2013 Nov 21.

Azaindoles: noncovalent DprE1 inhibitors from scaffold morphing efforts, kill Mycobacterium tuberculosis and are efficacious in vivo.

Author information

1
Department of Medicinal Chemistry, IMED Infection, AstraZeneca India , Bellary Road, Hebbal, Bangalore 560024, India.

Abstract

We report 1,4-azaindoles as a new inhibitor class that kills Mycobacterium tuberculosis in vitro and demonstrates efficacy in mouse tuberculosis models. The series emerged from scaffold morphing efforts and was demonstrated to noncovalently inhibit decaprenylphosphoryl-β-D-ribose2'-epimerase (DprE1). With "drug-like" properties and no expectation of pre-existing resistance in the clinic, this chemical class has the potential to be developed as a therapy for drug-sensitive and drug-resistant tuberculosis.

PMID:
24215368
DOI:
10.1021/jm401382v
[Indexed for MEDLINE]

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