A series of tripeptide arginine aldehydes was synthesized by replaceme
nt of proline with 1,2-disubstituted cyclohexane derivatives in the se
quence of D-MePhe-Pro-Arg-H. Based on molecular modeling, further modi
fication of the D-MePhe residue resulted in a potent and selective thr
ombin inhibitor. (C) 1998 Elsevier Science Ltd. All rights reserved.