2. Academic Validation
  3. Aryl piperazine melanocortin MC4 receptor agonists

Aryl piperazine melanocortin MC4 receptor agonists

  • Bioorg Med Chem Lett. 2003 Nov 3;13(21):3793-6. doi: 10.1016/s0960-894x(03)00796-0.
Brian Dyck 1,  Jessica Parker,  Teresa Phillips,  Lee Carter,  Brian Murphy,  Robin Summers,  Julia Hermann,  Tracy Baker,  Mary Cismowski,  John Saunders,  Val Goodfellow
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 10555 Science Center Drive, San Diego, CA 92121, USA.
PMID: 14552781 DOI: 10.1016/s0960-894x(03)00796-0
Abstract

Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC(50)=24 nM) and selective MC4-R agonists. We report the SAR of this series of compounds using in vitro cAMP functional assays in cells transfected with the MC4 or Other melancortin receptors.

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