Potent and selective thrombin inhibitors featuring hydrophobic, basic P₃-P₄-aminoalkyllactam moieties

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• 作者：Semple ; J. Edward ; Rowley ; David C. ; Owens ; Timothy D. ; Minami ; Nathaniel K. ; Uong ; Theresa H. ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1998
• 出版时间：December 15, 1998
• 年：1998
• 卷：8
• 期：24
• 页码：3525-3530
• 全文大小：315 K

文摘

Crystal structure and evolving SAR considerations of potent, selective benzylsulfonamide lactam thrombin inhibitors and related serine protease inhibitors have led to the design of novel thrombin inhibitors 1a-g, featuring hydrophobic, basic, P₄-alkylaminolactam scaffolds that serve as novel types of P₃-P₄ dipeptide mimics. The design, synthesis, and biological activity of these targets is presented.