title: Amino acid conjugates as kappa opioid receptor agonists.
abstract: A novel series of kappa (kappa) opioid receptor agonists were synthesized by incorporating the key structural features of known kappa opioid agonists while replacing the aryl acetamide portion with substituted amino acid conjugates. Compounds 3j (Ki = 6.7 nM), 3k (Ki = 3.6 nM), 3l (Ki = 4.6 nM), 3m (Ki = 0.83 nM) and 3o (Ki = 2 nM) possessed potent affinities for the kappa opioid receptor in vitro with reasonable selectivity over other opioid receptors.
authors.affiliation: Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. vkumar@adolor.com
authors.forename: Virendra
authors.initials: V
authors.lastname: Kumar
authors.forename: Deqi
authors.initials: D
authors.lastname: Guo
authors.forename: Jeffrey D
authors.initials: JD
authors.lastname: Daubert
authors.forename: Joel A
authors.initials: JA
authors.lastname: Cassel
authors.forename: Robert N
authors.initials: RN
authors.lastname: DeHaven
authors.forename: Erik
authors.initials: E
authors.lastname: Mansson
authors.forename: Diane L
authors.initials: DL
authors.lastname: DeHaven-Hudkins
authors.forename: Alan L
authors.initials: AL
authors.lastname: Maycock
mesh_terms: D000596:Amino Acids / Q000138:chemical synthesis* / Q000737:chemistry*; D006801:Humans; D015394:Molecular Structure; D017473:Receptors, Opioid, kappa / Q000819:agonists*
chemical_list: D000596:Amino Acids; D017473:Receptors, Opioid, kappa