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2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists

Authors :
George A. Doss
Lex H.T. Van der Ploeg
Qianping Peng
Ravi P. Nargund
Charles Rosenblum
Randall R. Miller
Aurawan Vongs
Palucki Brenda
Tanya MacNeil
Ralph A. Stearns
Min K. Park
David H. Weinberg
Rui Tang
Arthur A. Patchett
Constantin Tamvakopoulos
Source :
Bioorganic & Medicinal Chemistry Letters. 15:1993-1996
Publication Year :
2005
Publisher :
Elsevier BV, 2005.

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.

Details

ISSN :
0960894X
Volume :
15
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....44e32b60eac4ad2438147bfe723f3834
Full Text :
https://doi.org/10.1016/j.bmcl.2005.02.068