Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides.
A new class of benzimidazole-5-sulfonamides has been identified as nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Initial structure-activity relationships are presented resulting in compounds 19 and 28 with submicromolar dual functional activity on human and rat receptors.
Hashimoto
Kentaro
K
Department of Chemistry, Research Center Kyoto, Bayer Yakuhin, Ltd, Kizu, Soraku, Kyoto 619-0216, Japan. kentaro.hashimoto@bayerhealthcare.com
Tatsuta
Miyuki
M
Kataoka
Mikayo
M
Yasoshima
Kayo
K
Shogase
Yuka
Y
Shimazaki
Makoto
M
Yura
Takeshi
T
Li
Yingfu
Y
Yamamoto
Noriyuki
N
Gupta
Jang B
JB
Urbahns
Klaus
K
D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D007987:Gonadotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D051381:Rats; D013329:Structure-Activity Relationship
D001562:Benzimidazoles; D008024:Ligands; D007987:Gonadotropin-Releasing Hormone; C031000:benzimidazole