Potent and selective thrombin inhibitors featuring hydrophobic, basic P3P4-aminoalkyllactam moieties |
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Authors: | JEdward Semple David C Rowley Timothy D Owens Nathaniel K Minami Theresa H Uong Terence K Brunck |
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Institution: | Department of Medicinal Chemistry, Corvas International, Inc. 3030 Science Park Road, San Diego, CA 92121, USA |
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Abstract: | 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. |
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