title: Privileged structure-based ligands for melanocortin receptors-tetrahydroquinolines, indoles, and aminotetralines.
abstract: Substitution of the aryl sulfonamide moiety contained in MC4 agonist 1 with bicyclic heterocycles and aminotetralines produced compounds with MC4 activity. The heterocycles represent alternative privileged structures to that contained in 1. Compounds in which the polar group of the privileged structure was displayed in an endocyclic fashion were not as active as the parent agonist 1, while those with an exocyclic polar group afforded activity competitive with 1.
authors.affiliation: Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46258, USA. fisher_matthew_j@lilly.com
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Fisher
authors.forename: Ryan T
authors.initials: RT
authors.lastname: Backer
authors.forename: Saba
authors.initials: S
authors.lastname: Husain
authors.forename: Hansen M
authors.initials: HM
authors.lastname: Hsiung
authors.forename: Jeffrey T
authors.initials: JT
authors.lastname: Mullaney
authors.forename: Thomas P
authors.initials: TP
authors.lastname: O'Brian
authors.forename: Paul L
authors.initials: PL
authors.lastname: Ornstein
authors.forename: Roger R
authors.initials: RR
authors.lastname: Rothhaar
authors.forename: John M
authors.initials: JM
authors.lastname: Zgombick
authors.forename: Karin
authors.initials: K
authors.lastname: Briner
mesh_terms: D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D008024:Ligands; D015394:Molecular Structure; D011804:Quinolines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D044101:Receptors, Melanocortin / Q000187:drug effects* / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D007211:Indoles; D008024:Ligands; D011804:Quinolines; D044101:Receptors, Melanocortin; D013764:Tetrahydronaphthalenes