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.

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.

Bioorganic & medicinal chemistry letters (2004-12-08)

Brenda L Palucki, 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

PMID15582434

摘要

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.