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

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

Research output: Contribution to journalArticlepeer-review

25 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)2073-2077
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number16
DOIs
Publication statusPublished - Aug 19 2002
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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