Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus
| Autor: | Mark T. Goulet, Patrice H. Gibbons, Yi Tien Yang, Wallace T. Ashton, Kang Cheng, George R. Mount, Bridget Butler, Rosemary Sisco, Jane-Ling Lo, Joel B. Yudkovitz, Rena Ning Ren |
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| Rok vydání: | 2001 |
| Předmět: |
Indoles
Pyridines Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Carboxamide CHO Cells Alkylation Biochemistry Chemical synthesis chemistry.chemical_compound Cricetinae Drug Discovery Pyridine Side chain medicine Animals Humans Molecular Biology Indole test Bicyclic molecule Chemistry Organic Chemistry Amides Rats Molecular Medicine Amine gas treating Receptors LHRH |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 11:1727-1731 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(01)00275-x |
| Popis: | A pyridine side-chain terminus has been incorporated into the indole-5-carboxamide and indole-5-acetamide series of GnRH antagonists. Potent activity was observed in binding and functional assays. Certain branched or cyclic tertiary amides were identified as preferred in each series. Alkylation of the side-chain secondary amine had generally unfavorable effects. Variations of the gem-dialkyl substituents in the indole-5-acetamide series were also investigated. |
| Databáze: | OpenAIRE |
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