期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 8, 页码 2372-2375出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.11.055
关键词
tetracycline derivatives; anti-HIV activity; antimycobacterial activity; HIV-1 integrase
A series of new tetracycline derivatives has been synthesized by reacting appropriate tetracyclines, formaldehyde and secondary amino (piperazino) function of fluoroquinolones using microwave irradiation with the yield ranging from 41 evaluated for its anti-HIV, antimycobacterial activities and HIV-1 integrase (IN) enzyme inhibition studies. Among the synthesized compounds, compound 10 was found to be the most promising compound active against HIV-1 replication with EC50 of 5.2 mu M and was nontoxic to the CEM cells untill 200 mu M, and MIC of 0.2 mu g/mL against Mycobacterium tuberculosis, with moderate inhibition of both 3'-processing and strand transfer steps of HIV-1 IN. (c) 2007 Published by Elsevier Ltd.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据