The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.
Utilizing X-ray crystallography and molecular modeling, highly potent and selective peptidomimetic thrombin inhibitors have been designed containing a rigid piperazinedione template. The synthesis and biological activity of these compounds will be described.
Cody
W L
WL
Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Cai
C
C
Doherty
A M
AM
Edmunds
J J
JJ
He
J X
JX
Narasimhan
L S
LS
Plummer
J S
JS
Rapundalo
S T
ST
Rubin
J R
JR
Van Huis
C A
CA
St-Denis
Y
Y
Winocour
P D
PD
Siddiqui
M A
MA
D000991:Antithrombins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D015195:Drug Design; D008958:Models, Molecular; D010879:Piperazines / Q000737:chemistry*
D000991:Antithrombins; D010879:Piperazines