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

  作者 Chen, XW; Zhan, P; Pannecouque, C; Balzarini, J; De Clercq, E; Liu, XY  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2012年51-1;  页码  60-66  
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[摘要]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 wildtype 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. (C) 2012 Elsevier Masson SAS. All rights reserved.

 
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