Author/Authors :
Miyuki Tatsuta، نويسنده , , Mikayo Kataoka، نويسنده , , Kayo Yasoshima، نويسنده , , Sachiko Sakakibara، نويسنده , , Yuka Shogase، نويسنده , , Makoto Shimazaki، نويسنده , , Takeshi Yura، نويسنده , , Yingfu Li، نويسنده , , Noriyuki Yamamoto ، نويسنده , , Jang Gupta، نويسنده , , Klaus Urbahns، نويسنده ,
Abstract :
1-(1H-Benzimidazol-5-yl)-3-tert-butylurea derivatives have been identified as a novel class of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Herein, we disclose the synthesis and structure–activity relationships (SAR) of this class resulting in the identification of compound 12c, with dual functional activity on human and rat receptors (rat LHRH: IC50 = 120 nM; human LHRH: IC50 = 18 nM). These SAR studies suggest that 1-(1H-benzimidazol-5-yl)-3-tert-butylurea is a new pharmacophore for small molecule LHRH antagonists.
