title: High-throughput synthesis optimization of sulfonamide NPY Y5 antagonists.
abstract: A series of sulfonamide neuropeptide Y Y5 antagonists was optimized by preparation of sets of analogues using high-throughput synthesis and purification techniques. Testing of these compounds for their ability to bind to the human NPY Y5 receptor revealed separate SAR trends for sulfonamide amides versus sulfonamide ureas versus sulfonamide amines. By understanding these SAR trends, potent compounds were identified in all three series.
authors.affiliation: Synaptic Pharmaceutical Corporation, 215 College Road, Paramus, NJ 07952, USA. john.finn@cubist.com
authors.forename: John
authors.initials: J
authors.lastname: Finn
authors.forename: David
authors.initials: D
authors.lastname: Pelham
authors.forename: Mary W
authors.initials: MW
authors.lastname: Walker
authors.forename: Charles
authors.initials: C
authors.lastname: Gluchowski
mesh_terms: D000588:Amines / Q000737:chemistry; D000818:Animals; D019556:COS Cells; D002462:Cell Membrane / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D011485:Protein Binding; D011869:Radioligand Assay; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D014508:Urea / Q000031:analogs & derivatives / Q000737:chemistry
chemical_list: D000588:Amines; D017476:Receptors, Neuropeptide Y; D013449:Sulfonamides; C100568:neuropeptide Y5 receptor; D014508:Urea