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 c  Log  P s 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).