title: N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1.
abstract: Starting from a low micromolar agonist lead identified by high-throughput screening, series of N-isoquinolin-5-yl-N'-aralkyl ureas and analogous amides were developed as potent antagonists of human vanilloid receptor 1 (VR1). The synthesis and structure-activity relationships (SAR) of the series are described.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, Welsh and McKean Roads, Spring House, PA 19477, USA.
authors.forename: Michele C
authors.initials: MC
authors.lastname: Jetter
authors.forename: Mark A
authors.initials: MA
authors.lastname: Youngman
authors.forename: James J
authors.initials: JJ
authors.lastname: McNally
authors.forename: Sui-Po
authors.initials: SP
authors.lastname: Zhang
authors.forename: Adrienne E
authors.initials: AE
authors.lastname: Dubin
authors.forename: Nadia
authors.initials: N
authors.lastname: Nasser
authors.forename: Scott L
authors.initials: SL
authors.lastname: Dax
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000378:metabolism; D002460:Cell Line; D006801:Humans; D007546:Isoquinolines / Q000737:chemistry* / Q000378:metabolism; D011955:Receptors, Drug / Q000037:antagonists & inhibitors* / Q000378:metabolism; D050916:TRPV Cation Channels; D014508:Urea / Q000737:chemistry* / Q000378:metabolism
chemical_list: D000577:Amides; D007546:Isoquinolines; D011955:Receptors, Drug; D050916:TRPV Cation Channels; C494484:TRPV1 receptor; D014508:Urea