2. Academic Validation
  3. 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

  • Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5. doi: 10.1016/j.bmcl.2004.10.020.
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

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. brenda_palucki@merck.com
PMID: 15582434 DOI: 10.1016/j.bmcl.2004.10.020
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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