title: Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides.
abstract: 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.
authors.affiliation: Department of Chemistry, Research Center Kyoto, Bayer Yakuhin, Ltd, Kizu, Soraku, Kyoto 619-0216, Japan. kentaro.hashimoto@bayerhealthcare.com
authors.forename: Kentaro
authors.initials: K
authors.lastname: Hashimoto
authors.forename: Miyuki
authors.initials: M
authors.lastname: Tatsuta
authors.forename: Mikayo
authors.initials: M
authors.lastname: Kataoka
authors.forename: Kayo
authors.initials: K
authors.lastname: Yasoshima
authors.forename: Yuka
authors.initials: Y
authors.lastname: Shogase
authors.forename: Makoto
authors.initials: M
authors.lastname: Shimazaki
authors.forename: Takeshi
authors.initials: T
authors.lastname: Yura
authors.forename: Yingfu
authors.initials: Y
authors.lastname: Li
authors.forename: Noriyuki
authors.initials: N
authors.lastname: Yamamoto
authors.forename: Jang B
authors.initials: JB
authors.lastname: Gupta
authors.forename: Klaus
authors.initials: K
authors.lastname: Urbahns
mesh_terms: 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
chemical_list: D001562:Benzimidazoles; D008024:Ligands; D007987:Gonadotropin-Releasing Hormone; C031000:benzimidazole