Tetrazole thioacetanilides: Potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant

详细信息    查看全文

• 作者：Ester Muraglia ; Olaf D. Kinzel ; Ralph Laufer ; Michael D. Miller ; Gregory Moyer ; Vandna Munshi ; Federica Orvieto ; Maria Cecilia Palumbi ; Giovanna Pescatore ; Michael Rowley et al.
• 关键词：HIV ; Non-nucleoside reverse transcriptase inhibitors ; Tetrazole thioacetanilides
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：15 May 2006
• 年：2006
• 卷：16
• 期：10
• 页码：2748-2752
• 全文大小：112 K

文摘

A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats.