Bioorganic and Medicinal Chemistry Letters p. 1543 - 1548 (1997)
Update date:2022-08-03
Topics: Synthesis Characterization In vitro Testing In Vivo Testing Structure-Activity Relationship (SAR)
Tamura, Susan Y.
Semple, J. Edward
Reiner, John E.
Goldman, Erick A.
Brunck, Terence K.
Lim-Wilby, Marguerita S.
Carpenter, Stephen H.
Rote, William E.
Oldeshulte, Gerard L.
Richard, Brigitte M.
Nutt, Ruth F.
Ripka, William C.
Several potent and selective inhibitors of thrombin incorporating novel heterocyclic peptide surrogates in the P3-P2 position of peptidyl argininals have been discovered. Illustrated in this article are three classes of heterocycles: pyridones, uracils, and pyrimidinones. The synthesis and biological activities of these unique aromatic heterocyclic derivatives are reported herein.
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