Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: Modulation at the N-portion and distal phenyl ring (Articolo in rivista)

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Label
  • Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: Modulation at the N-portion and distal phenyl ring (Articolo in rivista) (literal)
Anno
  • 2013-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/j.ejmech.2013.02.005 (literal)
Alternative label
  • Ortar G, Morera E, De Petrocellis L, Ligresti A, Schiano Moriello A, Morera L, Nalli M, Ragno R, Pirolli A, Di Marzo V. (2013)
    Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: Modulation at the N-portion and distal phenyl ring
    in European journal of medicinal chemistry; Elsevier Masson SAS, Issy les Moulineaux (Francia)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Ortar G, Morera E, De Petrocellis L, Ligresti A, Schiano Moriello A, Morera L, Nalli M, Ragno R, Pirolli A, Di Marzo V. (literal)
Pagina inizio
  • 118 (literal)
Pagina fine
  • 132 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 63 (literal)
Rivista
Note
  • Scopus (literal)
  • ubMe (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, 00185 Roma, Italy Endocannabinoid Research Group, Istituto di Cibernetica, Consiglio Nazionale Delle Ricerche, via dei Campi Flegrei 34, 80078 Pozzuoli, Napoli, Italy Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale Delle Ricerche, via dei Campi Flegrei 34, 80078 Pozzuoli, Napoli, Italy (literal)
Titolo
  • Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: Modulation at the N-portion and distal phenyl ring (literal)
Abstract
  • In the present study, we have further extended the structure-activity relationships for the tetrazolyl ureas class of compounds as potential FAAH and/or MAGL inhibitors, by replacing the dimethylamino group of the parent compounds 1 and 2 with bulkier groups or by introducing on the distal phenyl ring of 1 and 2 a selected set of substituents. Some of the new compounds (16, 20, 21, 25, and 28) inhibited FAAH potently (IC50 = 3.0-9.7 nM) and selectively (39- to more than 141-fold) over MAGL, while tetrazole 27 turned out to be a promising dual FAAH-MAGL inhibitor of potential therapeutic use. Covalent docking studies on FAAH indicated that the binding modes of tetrazoles 1-32 did not display a unique pattern. The ability of tetrazoles 1-32 to act as TRPV1 and TRPA1 modulators was also investigated. (literal)
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