从4,5,6,7-四氢-5-甲基咪唑并[4,5,1-jk](1,4)苯二氮䓬-2(1H)-酮（替博韦）到依曲韦林（TMC125）：对HIV-1逆转录酶非核苷抑制剂的十五年研究。 - Suppr

From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.

作者信息

De Corte Bart L

机构信息

Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, Welsh and McKean Roads, Spring House, Pennsylvania 19477-0776, USA.

出版信息

J Med Chem. 2005 Mar 24;48(6):1689-96. doi: 10.1021/jm040127p.

DOI:10.1021/jm040127p

PMID:15771411

Abstract

摘要

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From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.

J Med Chem. 2005 Mar 24;48(6):1689-96. doi: 10.1021/jm040127p.

Quantitative structure-activity relationship studies on anti-HIV-1 TIBO derivatives as inhibitors of viral reverse transcriptase.

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Bioorg Med Chem. 1999 Nov;7(11):2427-36. doi: 10.1016/s0968-0896(99)00198-4.

Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants.

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From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.

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