Author/Authors :
Brian M. Mathes، نويسنده , , Kevin J. Hudziak، نويسنده , , John M. Schaus، نويسنده , , Yao-Chang Xu، نويسنده , , Albert L. Lehninger, David L. Nelson, Michael M. Cox، نويسنده , , David B. Wainscott، نويسنده , , Suzanne E. Nutter، نويسنده , , Wendy H. Gough، نويسنده , , Theresa A. Branchek، نويسنده , , John M. Zgombick، نويسنده , , Sandra A. Filla، نويسنده ,
Abstract :
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-HT1F receptor agonist indole analogues, 1–3. The replacement proved to be effective, providing compounds with similar 5-HT1F 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-HT1F receptor agonist with the potential to treat acute migraine.
