Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands.
Design and synthesis of potent MC4 selective agonists based on cyclohexylpiperidine derived cyclic urea, oxazolidinones, and sulfonamide based privileged structures are disclosed.
Bakshi
Raman K
RK
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. Raman_bakshi@merck.com
Hong
Qingmei
Q
Tang
Rui
R
Kalyani
Rubana N
RN
Macneil
Tanya
T
Weinberg
David H
DH
Van der Ploeg
Lex H T
LH
Patchett
Arthur A
AA
Nargund
Ravi P
RP
D015195:Drug Design; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000378:metabolism*; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D008024:Ligands; C470072:MC4R protein, human; D044105:Receptor, Melanocortin, Type 4