Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.
Zhang
H C
HC
The R. W. Johnson Pharmaceutical Research Institute, Spring House, Pennsylvania 19477, USA. hzhang@prius.jnj.com
Derian
C K
CK
Andrade-Gordon
P
P
Hoekstra
W J
WJ
McComsey
D F
DF
White
K B
KB
Poulter
B L
BL
Addo
M F
MF
Cheung
W M
WM
Damiano
B P
BP
Oksenberg
D
D
Reynolds
E E
EE
Pandey
A
A
Scarborough
R M
RM
Maryanoff
B E
BE
D000800:Angioplasty, Balloon; D000818:Animals; D003251:Constriction, Pathologic; D005343:Fibrinolytic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006168:Guinea Pigs; D007191:Indazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018716:Molecular Mimicry; D009130:Muscle, Smooth / Q000187:drug effects / Q000473:pathology; D051381:Rats; D044463:Receptor, PAR-1; D018179:Receptors, Thrombin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D005343:Fibrinolytic Agents; D007191:Indazoles; D007211:Indoles; C424723:RWJ 58259; D044463:Receptor, PAR-1; D018179:Receptors, Thrombin; D014508:Urea