title: 2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
abstract: We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. The 5- and 6-alkylated piperazine compounds exhibit low bioactivation potential as measured by covalent binding in microsome preparations.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. brenda_palucki@merck.com <brenda_palucki@merck.com>
authors.forename: Brenda L
authors.initials: BL
authors.lastname: Palucki
authors.forename: Min K
authors.initials: MK
authors.lastname: Park
authors.forename: Ravi P
authors.initials: RP
authors.lastname: Nargund
authors.forename: Rui
authors.initials: R
authors.lastname: Tang
authors.forename: Tanya
authors.initials: T
authors.lastname: MacNeil
authors.forename: David H
authors.initials: DH
authors.lastname: Weinberg
authors.forename: Aurawan
authors.initials: A
authors.lastname: Vongs
authors.forename: Charles I
authors.initials: CI
authors.lastname: Rosenblum
authors.forename: George A
authors.initials: GA
authors.lastname: Doss
authors.forename: Randall R
authors.initials: RR
authors.lastname: Miller
authors.forename: Ralph A
authors.initials: RA
authors.lastname: Stearns
authors.forename: Qianping
authors.initials: Q
authors.lastname: Peng
authors.forename: Constantin
authors.initials: C
authors.lastname: Tamvakopoulos
authors.forename: Lex H T
authors.initials: LH
authors.lastname: Van der Ploeg
authors.forename: Arthur A
authors.initials: AA
authors.lastname: Patchett
mesh_terms: D006801:Humans; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4