Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties

Stefania Butini, Sandra Gemma, Margherita Brindisi, Samuele Maramai, Patrizia Minetti, Diana Celona, Raffaella Napolitano, Franco Borsini, Walter Cabri, Filomena Fezza, Lucio Merlini, Sabrina Dallavalle, Giuseppe Campiani, Mauro MacCarrone

Research output: Contribution to journalArticle

Abstract

We herein describe the systematic approach used to develop new analogues of compound 2, recently identified as a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Aiming at identifying new scaffolds endowed with improved drug disposition properties with respect to the phenylpyrrole-based lead, we subjected it to two different structural modification strategies. This process allowed the identification of derivatives 4b and 5c as potent, reversible and non-competitive FAAH inhibitors.

Original languageEnglish
Pages (from-to)492-495
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number2
DOIs
Publication statusPublished - Jan 15 2013

Keywords

  • Cannabinoid system
  • Drug disposition properties
  • Enzyme inhibitors
  • Fatty acid amide hydrolase (FAAH)
  • Solubility

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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  • Cite this

    Butini, S., Gemma, S., Brindisi, M., Maramai, S., Minetti, P., Celona, D., Napolitano, R., Borsini, F., Cabri, W., Fezza, F., Merlini, L., Dallavalle, S., Campiani, G., & MacCarrone, M. (2013). Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties. Bioorganic and Medicinal Chemistry Letters, 23(2), 492-495. https://doi.org/10.1016/j.bmcl.2012.11.035