Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group.
Costanzo
M J
MJ
Drug Discovery, R. W. Johnson Pharmaceutical Research Institute, Spring House, Pennsylvania 19477, USA.
Maryanoff
B E
BE
Hecker
L R
LR
Schott
M R
MR
Yabut
S C
SC
Zhang
H C
HC
Andrade-Gordon
P
P
Kauffman
J A
JA
Lewis
J M
JM
Krishnan
R
R
Tulinsky
A
A
D000595:Amino Acid Sequence; D000818:Animals; D001120:Arginine / Q000031:analogs & derivatives; D001665:Binding Sites; D002417:Cattle; D018360:Crystallography, X-Ray; D006146:Guanidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008969:Molecular Sequence Data; D015394:Molecular Structure; D009842:Oligopeptides / Q000494:pharmacology; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010875:Pipecolic Acids / Q000494:pharmacology; D011485:Protein Binding; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013449:Sulfonamides; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013917:Thrombin / Q000037:antagonists & inhibitors* / Q000737:chemistry; D014361:Trypsin Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D006146:Guanidines; D009842:Oligopeptides; D010455:Peptides; D010875:Pipecolic Acids; C100912:RWJ 50353; D015842:Serine Proteinase Inhibitors; D013449:Sulfonamides; D013844:Thiazoles; D014361:Trypsin Inhibitors; D001120:Arginine; D013917:Thrombin; C031942:argatroban; C064289:efegatran