title: The discovery of potent selective NPY Y(2) antagonists.
abstract: A series of small molecules with a piperidinyl core were synthesized and tested for binding affinity (IC50) at human Neuropeptide Y Y2 receptor. Various amide related analogs (ureas, reversed amides, and sulfonamides) were evaluated. Several potent and selective NPY Y2 antagonists were identified.
authors.affiliation: Janssen Research & Development LLC, 3210 Merryfield Row, San Diego, CA 92121, USA. wchai@its.jnj.com
authors.forename: Wenying
authors.initials: W
authors.lastname: Chai
authors.forename: Victoria D
authors.initials: VD
authors.lastname: Wong
authors.forename: Diane
authors.initials: D
authors.lastname: Nepomuceno
authors.forename: Pascal
authors.initials: P
authors.lastname: Bonaventure
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008861:Microsomes / Q000378:metabolism; D011485:Protein Binding; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D014508:Urea / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism
chemical_list: D000577:Amides; D017476:Receptors, Neuropeptide Y; D013449:Sulfonamides; C095889:neuropeptide Y2 receptor; D014508:Urea