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Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moiety

✍ Scribed by Susan Y. Tamura; Erick A. Goldman; Terence K. Brunck; William C. Ripka; J. Edward Semple

Publisher: Elsevier Science
Year: 1997
Tongue: English
Weight: 406 KB
Volume: 7
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(97)00004-8

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✦ Synopsis

Based on molecular modeling and judicious combination of the salient topographic features of the recently discovered P3-1actam 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.

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