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

作者：Fullam Elizabeth^*; Talbot James; Abuhammed Areej; Westwood Isaac; Davies Stephen G; Russell Angela J; Sim Edith

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(9): 2759-2764.

DOI：10.1016/j.bmcl.2013.02.052

• Arylamine N-acetyltransferase
• Mycobacterium marinum
• Mycobacterium tuberculosis
• Pyrazole
• Enzyme inhibition
• Drug discovery

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.

• 出版日期2013-5-1