Bioorganic and Medicinal Chemistry Letters p. 331 - 336 (1997)
Update date:2022-08-02
Topics:
Tamura, Susan Y.
Goldman, Erick A.
Brunck, Terence K.
Ripka, William C.
Semple, J. Edward
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.
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