Potent and selective thrombin inhibitors featuring hydrophobic, basic P3-P4-aminoalkyllactam moieties |
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Authors: | JE Semple DC Rowley TD Owens NK Minami TH Uong TK Brunck |
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Affiliation: | Department of Medicinal Chemistry, Corvas International, Inc., 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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