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Start Over Author "Shizuo Kasai" Journal bioorganicmedicinal chemistry letters
1 results on '"Shizuo Kasai"'

1. A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones

Author

Shuichi Furuya, Nobuo Cho, Shizuo Kasai, Masahiko Fujino, Satoshi Sasaki, Yoshiaki Shimizu, Toshihiro Imaeda, Masataka Harada, Nobuhiro Suzuki, and Yoji Hayase

Subjects
endocrine system, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Pyrimidinones, Peptide hormone, Biochemistry, Chemical synthesis, Binding, Competitive, Gonadotropin-Releasing Hormone, Structure-Activity Relationship, Drug Discovery, Humans, Receptor, Molecular Biology, Bicyclic molecule, Molecular Structure, Chemistry, Organic Chemistry, Antagonist, Small molecule, Drug Design, Molecular Medicine, Luteinizing hormone, Receptors, LHRH, Hormone
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.

Published
2002

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