Design and synthesis of triazolopyrimidine acylsulfonamides as novel anti-mycobacterial leads acting through inhibition of acetohydroxyacid synthase

作者：Patil Vikas; Kale Manoj; Raichurkar Anandkumar; Bhaskar Brahatheeswaran; Prahlad Dwarakanath; Balganesh Meenakshi; Nandan Santosh; Hameed P Shahul^*

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(9): 2222-2225.

DOI：10.1016/j.bmcl.2014.02.054

• Triazolopyrimidine acylsulfonamides
• Acetohydroxyacid synthase
• Antimycobacterial

Novel triazolopyrimidine acylsulfonamides class of antimycobacterial agents, which are mycobacterial acetohydroxyacid synthase (AHAS) inhibitors were designed by hybridization of known AHAS inhibitors such as sulfonyl urea and triazolopyrimidine sulfonamides. This Letter describes the synthesis and SAR studies of this class of molecules by variation of two parts of the molecule, the phenyl and triazolopyrimidine rings. SAR study describes optimisation of enzyme potency, whole cell potency and evidence of mechanism of action.

• 出版日期2014-5-1