A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones |
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Authors: | Sasaki Satoshi Imaeda Toshihiro Hayase Yoji Shimizu Yoshiaki Kasai Shizuo Cho Nobuo Harada Masataka Suzuki Nobuhiro Furuya Shuichi Fujino Masahiko |
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Affiliation: | Pharmaceutical Research Division, Takeda Chemical Industries, Ltd., 10 Wadai, Tsukuba, 300-4293, Ibaraki, Japan. sasaki_satoshi@takeda.co.jp |
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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. |
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