2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
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.
Palucki
Brenda L
BL
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. brenda_palucki@merck.com <brenda_palucki@merck.com>
Park
Min K
MK
Nargund
Ravi P
RP
Tang
Rui
R
MacNeil
Tanya
T
Weinberg
David H
DH
Vongs
Aurawan
A
Rosenblum
Charles I
CI
Doss
George A
GA
Miller
Randall R
RR
Stearns
Ralph A
RA
Peng
Qianping
Q
Tamvakopoulos
Constantin
C
Van der Ploeg
Lex H T
LH
Patchett
Arthur A
AA
D006801:Humans; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4