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吡唑并[3,4-d]嘧啶的简便一锅法合成及其抗分枝杆菌活性评价

Facile one-pot synthesis and antimycobacterial evaluation of pyrazolo[3,4-d]pyrimidines.

作者信息

Trivedi Amit, Dodiya Dipti, Surani Janak, Jarsania Samir, Mathukiya Hitesh, Ravat Naresh, Shah Viresh

机构信息

Chemical Research Laboratory, Department of Chemistry, Saurashtra University, Rajkot, India.

出版信息

Arch Pharm (Weinheim). 2008 Jul;341(7):435-9. doi: 10.1002/ardp.200800027.

Abstract

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.

摘要

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。

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