SAR studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists.
The discovery of the potency-enhancing effect of 5-substitutions on the novel 2-arylindoles as nonpeptidyl GnRH receptor antagonists led to the identification of several analogues with high affinities on the GnRH receptor. The syntheses and SARs of these 5-substituted-2-arylindole analogues are reported.
Chu
L
L
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. lin_chu@merck.com
Lo
J L
JL
Yang
Y T
YT
Cheng
K
K
Smith
R G
RG
Fisher
M H
MH
Wyvratt
M J
MJ
Goulet
M T
MT
D000818:Animals; D007211:Indoles / Q000494:pharmacology*; D051381:Rats; D011966:Receptors, LHRH / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D007211:Indoles; D011966:Receptors, LHRH