Bioorganic and Medicinal Chemistry Letters p. 2501 - 2506 (1998)
Update date:2022-08-03
Topics:
Semple, J. Edward
Potent serine protease inhibitor la featuring a hybrid P3-P4 quaternary lactam dipeptide surrogate was prepared based upon SAR and molecular modeling investigations and in order to further probe the S2/S3 thrombin and FXa subsites. An efficient and concise synthetic route to the key aminolactam intermediate 4 was developed. The design, synthesis, and biological activity of this target and its P3-P4 diastereomer 1b is presented.
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