Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides
2000
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- Autor(en) / Beteiligte
- Titel
- Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2000-03, Vol.10 (5), p.443-447
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2000
- Quelle
- Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/S0960-894X(00)00024-XTitel-ID: cdi_proquest_miscellaneous_71005058
- Format
- –
- Schlagworte
- Amides - chemical synthesis, Amides - pharmacology, Animals, Biological and medical sciences, CHO Cells, Cricetinae, Hormones. Endocrine system, Humans, Luteinizing Hormone - metabolism, Medical sciences, Pharmacology. Drug treatments, Phosphatidylinositols - metabolism, Quinolones - chemical synthesis, Quinolones - pharmacology, Rats, Receptors, LHRH - antagonists & inhibitors, Stereoisomerism, Structure-Activity Relationship