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. 2005 Jan 3;15(1):171-5.
doi: 10.1016/j.bmcl.2004.10.020.

Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist

Brenda L Palucki  1 , Min K Park, Ravi P Nargund, Zhixiong Ye, Iyassu K Sebhat, Patrick G Pollard, Rubana N Kalyani, Rui Tang, Tanya Macneil, David H Weinberg, Aurawan Vongs, Charles I Rosenblum, George A Doss, Randall R Miller, Ralph A Stearns, Qianping Peng, Constantin Tamvakopoulos, Erin McGowan, William J Martin, Joseph M Metzger, Cherrie A Shepherd, Alison M Strack, D Euan Macintyre, Lex H T Van der Ploeg, Arthur A Patchett
Affiliations

Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist

Brenda L Palucki et al. Bioorg Med Chem Lett. .

Abstract

We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. Further in vivo development of lead agonist, MB243, is disclosed.

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