Abstract
Based on SAR from bicyclic GnRH antagonists such as 6-aminomethyl-7-arylpyrrolo[1,2-a]pyrimid-4-ones (1) and 2-aryl-3-aminomethylimidazolo[1,2-a]pyrimid-5-ones (2a,b), a series of novel uracil compounds (4) were derived as the GnRH antagonists. Their syntheses and initial SAR are discussed herein. This is the first time that monocycle-based GnRH receptor antagonists are reported.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Drug Stability
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology
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In Vitro Techniques
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Metabolic Clearance Rate
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Mice
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Microsomes, Liver / metabolism
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry
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Pyrroles / pharmacology
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Receptors, LHRH / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
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Uracil / chemical synthesis*
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Uracil / chemistry
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Uracil / pharmacology
Substances
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Imidazoles
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Pyrroles
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Receptors, LHRH
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Uracil