Synthesis and biological evaluation of phosphonate analogues of nevirapine

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• 作者：Jay Parrish ; ^{Jay.Parrish@gilead.com} ; Leah Tong ; Michael Wang ; Xiaowu Chen ; Eric B. Lansdon ; Carina Cannizzaro ; Xubin Zheng ; Manoj C. Desai ; Lianhong Xu
• 关键词：HIV ; Reverse transcriptase ; Non-nucleoside reverse transcriptase inhibitors ; NNRTI
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 March, 2013
• 年：2013
• 卷：23
• 期：5
• 页码：1493-1497
• 全文大小：613 K

文摘

A series of nevirapine-based analogues containing the phosphonate functionality were prepared and evaluated in vitro against HIV RT. The effect of the phosphonate was evaluated against the wild type and Y181C HIV replication. An in vivo PK study was performed on a select analogue.