860638-54-6Relevant articles and documents
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 2: Benzimidazole-5-sulfonamides
Li, Yingfu,Kataoka, Mikayo,Tatsuta, Miyuki,Yasoshima, Kayo,Yura, Takeshi,Urbahns, Klaus,Kiba, Atsushi,Yamamoto, Noriyuki,Gupta, Jang B.,Hashimoto, Kentaro
, p. 805 - 807 (2005)
The 2-cyclopropyl substituted benzimidazole 2 has been used as a starting point for further optimization of an LHRH antagonist series. SAR studies revealed that a tert-butyl urea fragment connected through a simple carbon chain would improve activity. Further modification of the benzylsulfonamide moiety led to the discovery of 23 (IC50: 4.2 nM).
