Trivedi Amit, Dodiya Dipti, Surani Janak, Jarsania Samir, Mathukiya Hitesh, Ravat Naresh, Shah Viresh
Chemical Research Laboratory, Department of Chemistry, Saurashtra University, Rajkot, India.
Arch Pharm (Weinheim). 2008 Jul;341(7):435-9. doi: 10.1002/ardp.200800027.
The present article describes a facile one-pot synthesis of a series of eight pyrazolo[3,4-d]pyrimidines 4a-h which were evaluated for their in-vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using the Alamar-Blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in mg/mL. The compounds 4b, 4c, 4d, and 4g exhibited the best results (1.2 microg/mL) when compared with first-line drugs such as isoniazid (INH) and rifampicin (RIP). Therefore, this class of compounds could be a good starting point to develop new lead compounds in the treatment of multidrug-resistant tuberculosis.
本文描述了一系列8种吡唑并[3,4-d]嘧啶4a-h的简便一锅法合成,使用阿拉玛蓝药敏试验评估了它们对结核分枝杆菌H37Rv的体外抗菌活性,活性以毫克/毫升表示的最低抑菌浓度(MIC)。与一线药物如异烟肼(INH)和利福平(RIP)相比,化合物4b、4c、4d和4g表现出最佳结果(1.2微克/毫升)。因此,这类化合物可能是开发治疗耐多药结核病新先导化合物的良好起点。