Author/Authors :
Yingfu Li، نويسنده , , Mikayo Kataoka، نويسنده , , Miyuki Tatsuta، نويسنده , , Kayo Yasoshima، نويسنده , , Takeshi Yura، نويسنده , , Klaus Urbahns، نويسنده , , Atsushi Kiba، نويسنده , , Noriyuki Yamamoto ، نويسنده , , Jang B. Gupta، نويسنده , , Kentaro Hashimoto، نويسنده ,
Abstract :
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).
