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

A 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 as PowerPoint slide