2. Academic Validation
  3. Arylboronic acids as dual-action FAAH and TRPV1 ligands

Arylboronic acids as dual-action FAAH and TRPV1 ligands

  • Bioorg Med Chem Lett. 2016 Mar 1;26(5):1401-5. doi: 10.1016/j.bmcl.2016.01.071.
Enrico Morera 1,  Vincenzo Di Marzo 2,  Ludovica Monti 3,  Marco Allarà 2,  Aniello Schiano Moriello 2,  Marianna Nalli 3,  Giorgio Ortar 3,  Luciano De Petrocellis 4
Affiliations

Affiliations

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy. Electronic address: enrico.morera@uniroma1.it.
  • 2 Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, via Campi Flegrei 34, 80078 Pozzuoli (Napoli), Italy.
  • 3 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy.
  • 4 Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, via Campi Flegrei 34, 80078 Pozzuoli (Napoli), Italy. Electronic address: luciano.depetrocellis@icb.cnr.it.
PMID: 26850005 DOI: 10.1016/j.bmcl.2016.01.071
Abstract

A series of 31 arylboronic acids designed on the basis of the pharmacophore model for a variety of TRPV1 antagonists was prepared and tested on FAAH and TRPV1 channel. Four of them, that is, compounds 3c, 4a, 5a,b acted as dual FAAH/TRPV1 blockers with IC50 values between 0.56 and 8.11μM whereas ten Others (compounds 1c,f-i, 2c-f, 4b) inhibited FAAH and activated/desensitized TRPV1.

Keywords

Boronic acids; Dual-ligands; FAAH; Fatty acid amide hydrolase; TRPV1; Transient receptor potential vanilloid type-1 channel.

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