Article ID Journal Published Year Pages File Type
1366852 Bioorganic & Medicinal Chemistry Letters 2007 4 Pages PDF
Abstract

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 41evaluated 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 μM and was nontoxic to the CEM cells untill 200 μM, and MIC of 0.2 μg/mL against Mycobacterium tuberculosis, with moderate inhibition of both 3′-processing and strand transfer steps of HIV-1 IN.

Graphical abstractA series of tetracycline derivatives has been synthesized by reacting appropriate tetracyclines, formaldehyde and secondary amino (piperazino) function of fluoroquinolones using microwave irradiation. Compound 10 was found to be the most promising compound active against HIV-1 replication with EC50 of 5.2 μM and was nontoxic to the CEM cells untill 200 μM, and MIC of 0.2 μg/mL against Mycobacterium tuberculosis, with moderate inhibition of both 3′-processing and strand transfer steps of HIV-1 IN.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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