title: 5-(2'-Pyridyl)-2-aminothiazoles: alkyl amino sulfonamides and sulfamides as potent NPY(5) antagonists.
abstract: Synthesis, SAR and physico-chemical properties of an alkyl aminothiazole series 8 and 16 are described. 2-Pyridylaminothiazole based compounds such as 8c and 16a exhibit high affinity at the NPY(5) receptor with desirable cLogPs and solubilities. However, they also suffer from high in vitro and in vivo clearance. Compound 16a partially inhibits the feeding behavior elicited by i.c.v. injection of the selective NPY(5) agonist [cPP(1-7), NPY(19-23), Ala(31), Aib(32), Gln(34)]-human pancreatic polypeptide polypeptide (cPP).
authors.affiliation: Chemical & Pharmacokinetic Sciences, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA. matp@lundbeck.com
authors.forename: Mathivanan
authors.initials: M
authors.lastname: Packiarajan
authors.forename: Heather
authors.initials: H
authors.lastname: Coate
authors.forename: Mahesh
authors.initials: M
authors.lastname: Desai
authors.forename: Hermogenes N
authors.initials: HN
authors.lastname: Jimenez
authors.forename: Emily J
authors.initials: EJ
authors.lastname: Reinhard
authors.forename: Vrej J
authors.initials: VJ
authors.lastname: Jubian
authors.forename: Mohammad R
authors.initials: MR
authors.lastname: Marzabadi
authors.forename: Gamini
authors.initials: G
authors.lastname: Chandrasena
authors.forename: Toni C
authors.initials: TC
authors.lastname: Wolinski
authors.forename: Mary W
authors.initials: MW
authors.lastname: Walker
authors.forename: Kim
authors.initials: K
authors.lastname: Andersen
mesh_terms: D000818:Animals; D005247:Feeding Behavior / Q000187:drug effects; D006801:Humans; D007276:Injections, Intraventricular; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D012995:Solubility; D013449:Sulfonamides / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D017476:Receptors, Neuropeptide Y; D013449:Sulfonamides; C100568:neuropeptide Y5 receptor