Abstract
SAR studies which focused upon the C-6 position of a recently described series of quinolone gonadotropin releasing hormone antagonists are reported. Synthetic access to diverse quinolone-6-carboxamides was achieved via the palladium-catalyzed amino-carbonylation reactions of iodide 4 with various amines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors.
MeSH terms
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Amides / chemical synthesis*
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Amides / pharmacology
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Animals
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CHO Cells
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Cricetinae
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Humans
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Luteinizing Hormone / metabolism
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Phosphatidylinositols / metabolism
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Quinolones / chemical synthesis*
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Quinolones / pharmacology
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Rats
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Receptors, LHRH / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Amides
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Phosphatidylinositols
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Quinolones
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Receptors, LHRH
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Luteinizing Hormone