Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses

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• 作者：Guozhi Tang ; Denis J. Kertesz ; Minmin Yang ; Xianfeng Lin ; Zhanguo Wang ; Wentao Li ; Zongxing Qiu ; Junli Chen ; Jianghua Mei ; Li Chen ; Taraneh Mirzadegan ; Seth F. Harris ; Arm ; o G. Villaseñ ; or ; Jennif
• 关键词：Non-nucleoside reverse transcriptase ; Non-nucleoside reverse transcriptase inhibitor (NNRTI) ; HIV-1
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 October 2010
• 年：2010
• 卷：20
• 期：20
• 页码：6020-6023
• 全文大小：626 K

文摘

Further investigation of the recently reported piperidine-4-yl-aminopyrimidine class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been carried out. Thus, preparation of a series of N-phenyl piperidine analogs resulted in the identification of 3-carboxamides as a particularly active series. Analogs such as 28 and 40 are very potent versus wild-type HIV-1 and a broad range of NNRTI-resistant mutant viruses. Synthesis, structure–activity relationship (SAR), clearance data, and crystallographic evidence for the binding motif are discussed.