Abstract
Initial SAR studies on 1-aminomethyl-2-aryl-3-cyano-pyrrolo[1,2-a]pyrimid-7-one-6-carboxylates as human GnRH receptor antagonists were discussed. 2-(2-Methylaminoethyl)pyridine was discovered to be a key feature for generating active compounds. The best compound from the series had 25 nM (K(i)) binding affinity to human GnRH receptor.
MeSH terms
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Animals
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Humans
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Indicators and Reagents
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Kinetics
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Pyrimidinones / chemical synthesis*
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Pyrimidinones / pharmacology*
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Pyrroles / chemical synthesis*
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Pyrroles / pharmacology*
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Radioligand Assay
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Rats
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Receptors, LHRH / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Indicators and Reagents
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Pyrimidinones
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Pyrroles
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Receptors, LHRH