The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.
Potent and selective thrombin inhibitors have been prepared with a piperazinedione template and L-amino acids. Likewise, incorporation of D-amino acids led to potent inhibitors with a novel mode of binding. Herein, the structure activity relationships and structural aspects of these compounds will be described.
Cody
W L
WL
Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Augelli-Szafran
C E
CE
Berryman
K A
KA
Cai
C
C
Doherty
A M
AM
Edmunds
J J
JJ
He
J X
JX
Narasimhan
L S
LS
Penvose-Yi
J
J
Plummer
J S
JS
Rapundalo
S T
ST
Rubin
J R
JR
Van Huis
C A
CA
Leblond
L
L
Winocour
P D
PD
Siddiqui
M A
MA
D000991:Antithrombins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D015195:Drug Design; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000991:Antithrombins; D010879:Piperazines