… design, synthesis, and serine protease inhibitory activity of a novel P 1-argininal derivative featuring a conformationally constrained P 2–P 3 bicyclic lactam moiety

SY Tamura, EA Goldman, TK Brunck, WC Ripka…

文献索引：Tamura, Susan Y.; Goldman, Erick A.; Brunck, Terence K.; Ripka, William C.; Semple, J. Edward Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 3 p. 331 - 336

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被引用次数: 38

摘要

Based on molecular modeling and judicious combination of the salient topographic features of the recently discovered P3-lactam derivative 1 with the P2-prolyl derivatives 2a, b, the novel thrombin inhibitor 3a was designed. Inhibitor 3a incorporates a fused bicyclic lactam as a novel type of P2–P3 dipeptide surrogate. The synthesis and biological activity of this potent serine protease inhibitor is presented.