Novel thombin inhibitors that are based on a macrocyclic tripeptide motif

DOI: 10.1016/S0960-894X(96)00554-9

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2947 - 2952 (1996)

Update date:2022-07-30

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Authors:

Greco, Michael N.

Powell, Eugene T.

Hecker, Leonard R.

Andrade-Gordon, Patricia

Kauffman, Jack A.

Lewis, Joan M.

Ganesh, Venkatapathy

Tulinsky, Alexander

Maryanoff, Bruce E.

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Article abstract of DOI:10.1016/S0960-894X(96)00554-9

A series of macrocyclic α-keto amides containing the D-Phe-Pro-Arg (fPR) motif were synthesized and evaluated in vitro as inhibitors of human α-thrombin and bovine trypsin. Structure-function studies, relating ring size and modifications at the P3 and P1' positions to enzyme inhibition, are described. An X-ray crystallographic study was performed on a ternary complex from 3i, thrombin, and hirugen.

Full text of DOI:10.1016/S0960-894X(96)00554-9

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