187155-14-2Relevant academic research and scientific papers
Novel thombin inhibitors that are based on a macrocyclic tripeptide motif
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.
, p. 2947 - 2952 (2007/10/03)
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.
