title: 3-Acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists.
abstract: A series of 3-acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid were designed and synthesized as vanilloid receptor agonists containing the three principal pharmacophores of resiniferatoxin. Amide analogues 23, 5 and 11 were found to be potent agonists in vanilloid receptor assay both for ligand binding and for activation.
authors.affiliation: Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, Korea.
authors.forename: J
authors.initials: J
authors.lastname: Lee
authors.forename: S U
authors.initials: SU
authors.lastname: Park
authors.forename: J Y
authors.initials: JY
authors.lastname: Kim
authors.forename: J K
authors.initials: JK
authors.lastname: Kim
authors.forename: J
authors.initials: J
authors.lastname: Lee
authors.forename: U
authors.initials: U
authors.lastname: Oh
authors.forename: V E
authors.initials: VE
authors.lastname: Marquez
authors.forename: M
authors.initials: M
authors.lastname: Beheshti
authors.forename: Q J
authors.initials: QJ
authors.lastname: Wang
authors.forename: S
authors.initials: S
authors.lastname: Modarres
authors.forename: P M
authors.initials: PM
authors.lastname: Blumberg
mesh_terms: D000577:Amides / Q000737:chemistry*; D015195:Drug Design; D004952:Esters / Q000737:chemistry*; D006719:Homovanillic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D011955:Receptors, Drug / Q000819:agonists*
chemical_list: D000577:Amides; D004952:Esters; D011955:Receptors, Drug; D006719:Homovanillic Acid