Newer tetracycline derivatives: Synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase

被引：35

作者：

Sriram, Dharmarajan ^{[1
]}

Yogeeswari, Perumal ^{[1
]}

Senchani, Geetha ^{[1
]}

Banerjee, Debjani ^{[1
]}

机构：

[1] Birla Inst Technol & Sci, Pharm Grp, Med Chem Res Lab, Pilani 333031, Rajasthan, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 08期

关键词：

tetracycline derivatives; anti-HIV activity; antimycobacterial activity; HIV-1; integrase; SPECTRUM CHEMOTHERAPEUTIC PROPERTIES; HUMAN-IMMUNODEFICIENCY-VIRUS; TUBERCULOSIS; MORTALITY;

D O I：

10.1016/j.bmcl.2006.11.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：2372 / 2375

页数：4

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