title: Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
abstract: Discovery of a series of tert-butyl pyrrolidine derived, potent and orally bioavailable melanocortin receptor subtype-4 (MC4R) selective modulators is disclosed.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, 126 E. Lincoln Avenue, PO Box 2000, RY 50G-332, Rahway, NJ 07065, USA. liangqin_guo@merck.com
authors.forename: Liangqin
authors.initials: L
authors.lastname: Guo
authors.forename: Zhixiong
authors.initials: Z
authors.lastname: Ye
authors.forename: Feroze
authors.initials: F
authors.lastname: Ujjainwalla
authors.forename: Heather L
authors.initials: HL
authors.lastname: Sings
authors.forename: Iyassu K
authors.initials: IK
authors.lastname: Sebhat
authors.forename: John
authors.initials: J
authors.lastname: Huber
authors.forename: David H
authors.initials: DH
authors.lastname: Weinberg
authors.forename: Rui
authors.initials: R
authors.lastname: Tang
authors.forename: Tanya
authors.initials: T
authors.lastname: MacNeil
authors.forename: Constantin
authors.initials: C
authors.lastname: Tamvakopoulos
authors.forename: Qianping
authors.initials: Q
authors.lastname: Peng
authors.forename: Euan
authors.initials: E
authors.lastname: MacIntyre
authors.forename: Lex H T
authors.initials: LH
authors.lastname: van der Ploeg
authors.forename: Mark T
authors.initials: MT
authors.lastname: Goulet
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: Ravi P
authors.initials: RP
authors.lastname: Nargund
mesh_terms: D000284:Administration, Oral; D006801:Humans; D015394:Molecular Structure; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D019098:Telomerase
chemical_list: D011759:Pyrrolidines; D044105:Receptor, Melanocortin, Type 4; C509186:TERT protein, human; D019098:Telomerase