Faculty of Science
Microbiology and Immunology

5-Carboxamide-substituted barbituric acids: Promising scaffolds for drug development against Mycobacterium tuberculosis

A schematic of drug development

Publication Date

Publication Journal

ACS Infectious Diseases

Author(s)

Henok A. Sahile, Bhuwan Awasthi, Jonas E. Olsen; Houria Afshar, Sung-Won Kim, Itay Amrom, Zohra Nikjo, Leah Rankine-Wilson, Wayne W. H. Law, Selvarani Vimalanathan, Clement K. M. Tsui, John L. Rubinstein, Brent D.G. Page, and Yossef Av-Gay

Mycobacterium tuberculosis (Mtb), the bacterium that causes tuberculosis, is resistant to many traditional antibiotics, necessitating new classes of drugs with unique mechanisms. In this study, the authors  screened a library of compounds and discovered that fenoxacrim displayed potent activity against Mtb by inhibiting an enzyme that helps to build the bacterial cell wall. The team used medicinal chemistry to develop analogues with enhanced selectivity and potency toward Mtb and reduced cytotoxicity, establishing a promising scaffold for antimicrobial drug development.

  • Av-Gay Lab

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Microbiology and Immunology

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