2. Academic Validation
  3. Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors

Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors

  • Eur J Med Chem. 2012 May:51:60-6. doi: 10.1016/j.ejmech.2012.02.019.
Xuwang Chen 1,  Peng Zhan,  Christophe Pannecouque,  Jan Balzarini,  Erik De Clercq,  Xinyong Liu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012 Ji'nan, Shandong, PR China.
PMID: 22405288 DOI: 10.1016/j.ejmech.2012.02.019
Abstract

A novel series of piperidine-substituted triazine derivatives have been synthesized and evaluated for anti-HIV activities in MT-4 cells. Most compounds displayed extremely promising activity against wild-type HIV-1 with EC(50) values in low nanomolar concentration, better than that of Nevirapine, Delavirdine, Zidovudine and Dideoxycitidine, and higher potency towards the resistant mutant strain K103N/Y181C than that of Nevirapine and Delavirdine. Selected compounds were also assayed against Reverse Transcriptase with lower IC(50) values than that of Nevirapine. The structure-activity relationship (SAR) of these novel structural congeners was also discussed.

Figures