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

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2372-5. doi: 10.1016/j.bmcl.2006.11.055.

Dharmarajan Sriram ¹, Perumal Yogeeswari, Geetha Senchani, Debjani Banerjee

Affiliations

Affiliation

1 Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333031, India. dsiram@bits-pilani.ac.in

PMID: 17376679 DOI: 10.1016/j.bmcl.2006.11.055

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 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 EC(50) of 5.2 microM and was nontoxic to the CEM cells until 200 microM, and MIC of 0.2 microg/mL against Mycobacterium tuberculosis, with moderate inhibition of both 3'-processing and strand transfer steps of HIV-1 IN.

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