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The synthesis and inhibitory potencies of a novel series of 3,5-diaryl-1H-pyrazoles as specific inhibitors of prokaryotic arylamine N-acetyltransferase enzymes is described. The series is based on hit compound 1 3,5-diaryl-1H-pyrazole identified from a high-throughout screen that has been carried out previously and found to inhibit the growth of Mycobacterium tuberculosis.

Original publication

DOI

10.1016/j.bmcl.2013.02.052

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/05/2013

Volume

23

Pages

2759 - 2764

Keywords

Antitubercular Agents, Arylamine N-Acetyltransferase, Binding Sites, Drug Design, Enzyme Inhibitors, Molecular Docking Simulation, Mycobacterium tuberculosis, Protein Structure, Tertiary, Pyrazoles, Structure-Activity Relationship