Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides

Kentaro Hashimoto; Miyuki Tatsuta; Mikayo Kataoka; Kayo Yasoshima; Yuka Shogase; Makoto Shimazaki; Takeshi Yura; Yingfu Li; Noriyuki Yamamoto; Jang B Gupta; Klaus Urbahns

doi:10.1016/j.bmcl.2004.10.089

Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides

Bioorg Med Chem Lett. 2005 Feb 1;15(3):799-803. doi: 10.1016/j.bmcl.2004.10.089.

Authors

Kentaro Hashimoto¹, Miyuki Tatsuta, Mikayo Kataoka, Kayo Yasoshima, Yuka Shogase, Makoto Shimazaki, Takeshi Yura, Yingfu Li, Noriyuki Yamamoto, Jang B Gupta, Klaus Urbahns

Affiliation

¹ Department of Chemistry, Research Center Kyoto, Bayer Yakuhin, Ltd, Kizu, Soraku, Kyoto 619-0216, Japan. kentaro.hashimoto@bayerhealthcare.com

PMID: 15664860
DOI: 10.1016/j.bmcl.2004.10.089

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.

MeSH terms

Animals
Benzimidazoles / chemical synthesis*
Benzimidazoles / pharmacology*
Gonadotropin-Releasing Hormone / antagonists & inhibitors*
Humans
Inhibitory Concentration 50
Ligands
Rats
Structure-Activity Relationship

Substances

Benzimidazoles
Ligands
Gonadotropin-Releasing Hormone
benzimidazole