Substituted furo[3,2-b]pyridines: novel bioisosteres of 5-HT1F receptor agonists
| Autor: | David B. Wainscott, John Mehnert Schaus, Wendy H. Gough, Yao-Chang Xu, Brian Michael Mathes, John M. Zgombick, Sandra Ann Filla, David L. Nelson, Suzanne E. Nutter, Kevin John Hudziak, Theresa Branchek |
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| Rok vydání: | 2004 |
| Předmět: |
Indole test
Agonist Bicyclic molecule Pyridines Stereochemistry medicine.drug_class Organic Chemistry Clinical Biochemistry Pharmaceutical Science Carboxamide 5-HT1F receptor Biochemistry Chemical synthesis Serotonin Receptor Agonists chemistry.chemical_compound chemistry Receptors Serotonin Drug Discovery medicine Molecular Medicine Bioisostere Receptor Molecular Biology Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 14:167-170 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2003.09.091 |
| Popis: | Synthesis and evaluation of a series of 2,3,5- and 3,5-substituted furo[3,2- b ]pyridines were undertaken in order to investigate their utility as bioisosteres of 5-HT 1F receptor agonist indole analogues, 1 – 3 . The replacement proved to be effective, providing compounds with similar 5-HT 1F receptor affinity and improved selectivity when compared with the indole analogues. Through these studies we identified 4-fluoro- N -[3-(1-methyl-piperidin-4-yl)-furo[3,2- b ]pyridin-5-yl]-benzamide ( 5 ), a potent and selective 5-HT 1F receptor agonist with the potential to treat acute migraine. |
| Databáze: | OpenAIRE |
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