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.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacology*
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Cell Line
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Chemistry Techniques, Synthetic
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV-1 / drug effects*
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HIV-1 / enzymology
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Inhibitory Concentration 50
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Piperidines / chemistry*
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Reverse Transcriptase Inhibitors / chemical synthesis
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Reverse Transcriptase Inhibitors / chemistry
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Reverse Transcriptase Inhibitors / pharmacology*
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Structure-Activity Relationship
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Triazines / chemical synthesis*
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Triazines / chemistry
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Triazines / pharmacology*
Substances
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Anti-HIV Agents
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Piperidines
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Reverse Transcriptase Inhibitors
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Triazines
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piperidine
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HIV Reverse Transcriptase