Design, synthesis and structure-activity relationships of 3,5-diaryl-1H-pyrazoles as inhibitors of arylamine N-acetyltransferase.

Journal article

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.

Authors: Fullam, E; Talbot, J; Abuhammed, A; Westwood, I; Davies, S

• Publication status: Published
• Journal: Bioorganic and medicinal chemistry letters
• Volume: 23
• Issue: 9
• Pages: 2759-2764
• Publication date: 2013-05-01
• DOI: 10.1016/j.bmcl.2013.02.052
• EISSN: 1464-3405
• ISSN: 0960-894X
• Language: English
• Keywords: Enzyme Inhibitors; Molecular Docking Simulation; Arylamine N-Acetyltransferase; Pyrazoles; Mycobacterium tuberculosis; Structure-Activity Relationship; Protein Structure, Tertiary; Binding Sites; Antitubercular Agents; Drug Design