Novel indole sulfides as potent HIV-1 NNRTIs

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• 作者：Siobhan Brigg^a ; Nicole Pribut^a ; Adriaan E. Basson^b ; Moscos Avgenikos^a ; Reinhardt Venter^a ; Margaret A. Blackie^a ; Willem A.L. van Otterlo^a ; Stephen C. Pelly^a ; ^{scpelly@sun.ac.za" class="auth_mail" title="E-mail the corresponding author}
• 关键词：HIV ; NNRTI ; Indole ; Sulfides
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 March 2016
• 年：2016
• 卷：26
• 期：6
• 页码：1580-1584
• 全文大小：996 K

文摘

In a previous communication we described a series of indole based NNRTIs which were potent inhibitors of HIV replication, both for the wild type and K103N strains of the virus. However, the methyl ether functionality on these compounds, which was crucial for potency, was susceptible to acid promoted indole assisted S_N1 substitution. This particular problem did not bode well for an orally bioavailable drug. Here we describe bioisosteric replacement of this problematic functional group, leading to a series of compounds which are potent inhibitors of HIV replication, and are acid stable.