title: Privileged structure based ligands for melanocortin-4 receptors--aliphatic piperazine derivatives.
abstract: Aliphatic carbocyclic replacement of the benzyl group of compound 1 yielded compounds with high affinity for the melanocortin-4 receptor (MC4R). Compounds with a cyclohexyl group showed a consistent high affinity, while different polar groups with less basicity were good replacements for the original diethyl amines. Substitution of the polar group found in these privileged structures with an aliphatic moiety produced compounds with high affinity for MC4R.
authors.affiliation: Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46258, USA.
authors.forename: Karin
authors.initials: K
authors.lastname: Briner
authors.forename: Iván
authors.initials: I
authors.lastname: Collado
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Fisher
authors.forename: Cristina
authors.initials: C
authors.lastname: García-Paredes
authors.forename: Saba
authors.initials: S
authors.lastname: Husain
authors.forename: Steven L
authors.initials: SL
authors.lastname: Kuklish
authors.forename: Ana I
authors.initials: AI
authors.lastname: Mateo
authors.forename: Thomas P
authors.initials: TP
authors.lastname: O'Brien
authors.forename: Paul L
authors.initials: PL
authors.lastname: Ornstein
authors.forename: John
authors.initials: J
authors.lastname: Zgombick
authors.forename: Oscar
authors.initials: O
authors.lastname: de Frutos
mesh_terms: D008024:Ligands; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000187:drug effects* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4