Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.
SAR about the piperidine core in a series of MC4R agonists is described. A number of alkyl substituents that furnish compounds with good affinity and functional potency are reported.
Sebhat
Iyassu K
IK
Department of Medicinal Chemistry, Merck & Co., Inc, PO Box, 2000, Rahway, NJ 07065, USA. iyassu_sebhat@merck.com
Lai
Yingjie
Y
Barakat
Khaled
K
Ye
Zhixiong
Z
Tang
Rui
R
Kalyani
Rubana N
RN
Vongs
Aurawan
A
Macneil
Tanya
T
Weinberg
David H
DH
Cabello
M Angeles
MA
Maroto
Marta
M
Teran
Ana
A
Fong
Tung M
TM
Van der Ploeg
Lex H T
LH
Patchett
Arthur A
AA
Nargund
Ravi P
RP
D000473:Alkanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000577:Amides / Q000737:chemistry; D006801:Humans; D015394:Molecular Structure; D009570:Nitriles / Q000737:chemistry; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000737:chemistry
D000473:Alkanes; D000577:Amides; D009570:Nitriles; D010880:Piperidines; D044105:Receptor, Melanocortin, Type 4; D013777:Tetrazoles; C045574:1H-tetrazole; C032727:piperidine