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针对关键临床突变具有增强效力的二芳基醚第二代HIV-1非核苷逆转录酶抑制剂（NNRTIs）的设计与合成。

The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.

作者信息

Tucker Thomas J, Saggar Sandeep, Sisko John T, Tynebor Robert M, Williams Theresa M, Felock Peter J, Flynn Jessica A, Lai Ming-Tain, Liang Yuexia, McGaughey Georgia, Liu Meiquing, Miller Mike, Moyer Gregory, Munshi Vandna, Perlow-Poehnelt Rebecca, Prasad Sridhar, Sanchez Rosa, Torrent Maricel, Vacca Joseph P, Wan Bang-Lin, Yan Youwei

机构信息

Department of Medicinal Chemistry, Merck Research Laboratories, WP14-3, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, USA.

出版信息

Bioorg Med Chem Lett. 2008 May 1;18(9):2959-66. doi: 10.1016/j.bmcl.2008.03.064. Epub 2008 Mar 25.

DOI:10.1016/j.bmcl.2008.03.064
PMID:18396399
Abstract

Using a combination of traditional Medicinal Chemistry/SAR analysis, crystallography, and molecular modeling, we have designed and synthesized a series of novel, highly potent NNRTIs that possess broad antiviral activity against a number of key clinical mutations.

摘要

通过结合传统药物化学/构效关系分析、晶体学和分子建模，我们设计并合成了一系列新型的、高效的非核苷类逆转录酶抑制剂，它们对多种关键临床突变具有广泛的抗病毒活性。

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