CB2-Selective Cannabinoid Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Modeling Investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides. (Articolo in rivista)

Type

• Articolo in rivista (Classe)
• Prodotto della ricerca (Classe)

Label

• CB2-Selective Cannabinoid Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Modeling Investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides. (Articolo in rivista) (literal)

Anno

• 2014-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

• 10.1021/jm500807e (literal)

Alternative label

• Lucchesi, Valentina; Hurst, Dow P; Shore, Derek M; Bertini, Simone; Ehrmann, Brandie M; Allara, Marco; Lawrence, Lyle; Ligresti, Alessia; Minutolo, Filippo; Saccomanni, Giuseppe; Sharir, Haleli; Macchia, Marco; Di Marzo, Vincenzo; Abood, Mary E; Reggio, Patricia H; Manera, Clementina (2014)
  CB2-Selective Cannabinoid Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Modeling Investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides.
  in Journal of medicinal chemistry (Online)
  (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

• Lucchesi, Valentina; Hurst, Dow P; Shore, Derek M; Bertini, Simone; Ehrmann, Brandie M; Allara, Marco; Lawrence, Lyle; Ligresti, Alessia; Minutolo, Filippo; Saccomanni, Giuseppe; Sharir, Haleli; Macchia, Marco; Di Marzo, Vincenzo; Abood, Mary E; Reggio, Patricia H; Manera, Clementina (literal)

Pagina inizio

• 8777 (literal)

Pagina fine

• 91 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

• 57 (literal)

Rivista

• Journal of medicinal chemistry (Rivista)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo

• 21 (literal)

Note

• ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

• Consiglio Nazionale delle Ricerche (literal)

Titolo

• CB2-Selective Cannabinoid Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Modeling Investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides. (literal)

Abstract

• We have recently identified 1,8-naphthyridin-2(1H)-one-3-carboxamide as a new scaffold very suitable for the development of new CB2 receptor potent and selective ligands. In this paper we describe a number of additional derivatives in which the same central scaffold has been variously functionalized in position 1 or 6. All new compounds showed high selectivity and affinity in the nanomolar range for the CB2 receptor. Furthermore, we found that their functional activity is controlled by the presence of the substituents at position C-6 of the naphthyridine scaffold. In fact, the introduction of substituents in this position determined a functionality switch from agonist to antagonists/inverse agonists. Finally, docking studies showed that the difference between the pharmacology of these ligands may be in the ability/inability to block the Toggle Switch W6.48(258) (chi1 g+ trans) transition. (literal)

Prodotto di

• Struttura, funzione e \"profiling\" di endocannabinoidi e ammidi bioattive di acidi grassi implicati nelle patologie umane (PM.P01.012.001) (Modulo)
• Institute of biomolecular chemistry (ICB) (Istituto)

Autore CNR

• ALESSIA LIGRESTI (Unità di personale interno)

Incoming links:

Autore CNR di

• ALESSIA LIGRESTI (Unità di personale interno)

Prodotto

• Institute of biomolecular chemistry (ICB) (Istituto)
• Struttura, funzione e \"profiling\" di endocannabinoidi e ammidi bioattive di acidi grassi implicati nelle patologie umane (PM.P01.012.001) (Modulo)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi

• Journal of medicinal chemistry (Rivista)