Author/Authors :
Satoshi Sasaki، نويسنده , , Toshihiro Imaeda، نويسنده , , Yoji Hayase، نويسنده , , Yoshiaki Shimizu، نويسنده , , Shizuo Kasai، نويسنده , , Nobuo Cho، نويسنده , , Masataka Harada، نويسنده , , Nobuhiro Suzuki، نويسنده , , Shuichi Furuya، نويسنده , , Masahiko Fujino، نويسنده ,
Abstract :
The design and synthesis of a new class of nonpeptide luteinizing hormone-releasing hormone (LHRH) receptor antagonists, the 2-phenylimidazo[1,2-a]pyrimidin-5-ones, is reported. Among compounds described in this study, we identified the potent antagonist 15b with nanomolar in vitro functional antagonism. The result might suggest that the heterocyclic 5–6-ring system possessing a pendant phenyl group attached to the five-membered ring is the important structural feature for a scaffold of small molecule LHRH antagonists.
