Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands

Enrico Morera; Luciano De Petrocellis; Ludovica Morera; Aniello Schiano Moriello; Alessia Ligresti; Marianna Nalli; David F Woodward; Vincenzo Di Marzo; Giorgio Ortar

doi:10.1016/j.bmcl.2009.09.033

Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6806-9. doi: 10.1016/j.bmcl.2009.09.033. Epub 2009 Oct 20.

Authors

Enrico Morera¹, Luciano De Petrocellis, Ludovica Morera, Aniello Schiano Moriello, Alessia Ligresti, Marianna Nalli, David F Woodward, Vincenzo Di Marzo, Giorgio Ortar

Affiliation

¹ Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, 00185 Roma, Italy.

PMID: 19875281
DOI: 10.1016/j.bmcl.2009.09.033

Abstract

The evaluation of a series of piperazinyl carbamates and ureas, designed on the basis of previously reported TRPV1 antagonists and FAAH inhibitors, led to the identification of some 'dual-action' compounds targeting both FAAH and TRPV1 or TRPA1 receptors.

MeSH terms

Amidohydrolases / antagonists & inhibitors*
Carbamates / chemical synthesis*
Carbamates / chemistry
Carbamates / pharmacology*
Dose-Response Relationship, Drug
Drug Design
Ligands
Molecular Structure
Stereoisomerism
Structure-Activity Relationship
Transient Receptor Potential Channels / antagonists & inhibitors*
Urea / chemical synthesis*
Urea / chemistry
Urea / pharmacology*

Substances

Carbamates
Ligands
Transient Receptor Potential Channels
Urea
Amidohydrolases
fatty-acid amide hydrolase