TY - JOUR
T1 - A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists
T2 - Design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones
AU - Sasaki, Satoshi
AU - Imaeda, Toshihiro
AU - Hayase, Yoji
AU - Shimizu, Yoshiaki
AU - Kasai, Shizuo
AU - Cho, Nobuo
AU - Harada, Masataka
AU - Suzuki, Nobuhiro
AU - Furuya, Shuichi
AU - Fujino, Masahiko
PY - 2002/8/19
Y1 - 2002/8/19
N2 - 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.
AB - 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.
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U2 - 10.1016/S0960-894X(02)00372-4
DO - 10.1016/S0960-894X(02)00372-4
M3 - Article
C2 - 12127507
AN - SCOPUS:18444369293
SN - 0960-894X
VL - 12
SP - 2073
EP - 2077
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 16
ER -