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
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. [email protected]
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.