Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.
A series of 3-arylquinolones was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. A variety of substitution patterns of the 3-aryl substituent are described. The 3,4,5-trimethylphenyl substituent (23h) was found to be optimal.
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. jonathan_young@merck.com
J R
JR
Young
S X
SX
Huang
I
I
Chen
T F
TF
Walsh
R J
RJ
DeVita
M J
MJ
Wyvratt
M T
MT
Goulet
N
N
Ren
J
J
Lo
Y T
YT
Yang
J B
JB
Yudkovitz
K
K
Cheng
R G
RG
Smith
D007987:Gonadotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D015363:Quinolones; D007987:Gonadotropin-Releasing Hormone