Literature DB >> 14684321

Substituted furo[3,2-b]pyridines: novel bioisosteres of 5-HT 1F receptor agonists.

Brian M Mathes1, Kevin J Hudziak, John M Schaus, Yao-Chang Xu, David L Nelson, David B Wainscott, Suzanne E Nutter, Wendy H Gough, Theresa A Branchek, John M Zgombick, Sandra A Filla.   

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-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.

Entities:  

Mesh:

Substances:

Year:  2004        PMID: 14684321     DOI: 10.1016/j.bmcl.2003.09.091

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Parallel synthesis of a multi-substituted benzo[b]furan library.

Authors:  Chul-Hee Cho; Benjamin Neuenswander; Gerald H Lushington; Richard C Larock
Journal:  J Comb Chem       Date:  2008-10-21

2.  Bioisosteric matrices for ligands of serotonin receptors.

Authors:  Dawid Warszycki; Stefan Mordalski; Jakub Staroń; Andrzej J Bojarski
Journal:  ChemMedChem       Date:  2015-03-13       Impact factor: 3.466

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.