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A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones
- Source :
- Bioorganicmedicinal chemistry letters. 12(16)
- Publication Year :
- 2002
-
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.
- 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
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 12
- Issue :
- 16
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....f50a01adb9528dea81525dbd1df39ea3