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

被引：50

作者：

Chen, Xuwang ^{[1
]}

Zhan, Peng ^{[1
]}

Pannecouque, Christophe ^{[2
]}

Balzarini, Jan ^{[2
]}

De Clercq, Erik ^{[2
]}

Liu, Xinyong ^{[1
]}

机构：

[1] Shandong Univ, Dept Med Chem, Sch Pharmaceut Sci, Jinan 250012, Shandong, Peoples R China

[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 51卷

基金：

中国博士后科学基金; 中国国家自然科学基金; 高等学校博士学科点专项科研基金;

关键词：

HIV-1; NNRTIs; Piperidine; Triazine; AIDS; SAR; COLORIMETRIC ASSAY; BROAD POTENCY; DIARYLTRIAZINES; ETRAVIRINE; DISCOVERY; SERIES;

D O I：

10.1016/j.ejmech.2012.02.019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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 EC50 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 IC50 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.

引用

页码：60 / 66

页数：7

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