Document Report Card

Basic Information

ID: ALA1909589

Journal: Bioorg Med Chem Lett

Title: 5-(2'-Pyridyl)-2-aminothiazoles: alkyl amino sulfonamides and sulfamides as potent NPY(5) antagonists.

Authors: Packiarajan M, Coate H, Desai M, Jimenez HN, Reinhard EJ, Jubian VJ, Marzabadi MR, Chandrasena G, Wolinski TC, Walker MW, Andersen K.

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).

CiteXplore: 21924902

DOI: 10.1016/j.bmcl.2011.08.072