Tricyclic pyrazoles. Part 2: Synthesis and biological evaluation of novel 4,5-dihydro-1H-benzo[g]indazole-based ligands for cannabinoid receptors. (Articolo in rivista)

Type

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

Label

• Tricyclic pyrazoles. Part 2: Synthesis and biological evaluation of novel 4,5-dihydro-1H-benzo[g]indazole-based ligands for cannabinoid receptors. (Articolo in rivista) (literal)

Anno

• 2005-01-01T00:00:00+01:00 (literal)

Alternative label

• Murineddu G, Ruiu S, Mussinu JM, Loriga G, Grella GE, Carai MA, Lazzari P, Pani L, Pinna GA. (2005)
  Tricyclic pyrazoles. Part 2: Synthesis and biological evaluation of novel 4,5-dihydro-1H-benzo[g]indazole-based ligands for cannabinoid receptors.
  in Bioorganic & medicinal chemistry (Print)
  (literal)

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

• Murineddu G, Ruiu S, Mussinu JM, Loriga G, Grella GE, Carai MA, Lazzari P, Pani L, Pinna GA. (literal)

Pagina inizio

• 3309 (literal)

Pagina fine

• 3320 (literal)

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

• 13 (literal)

Rivista

• Bioorganic & medicinal chemistry (Rivista)

Note

• ISI Web of Science (WOS) (literal)

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

• Dipartimento Farmaco Chimico Tossicologico, Universita di Sassari, Neuroscienze PharmaNess SCARL,Cagliari, Italy. (literal)

Titolo

• Tricyclic pyrazoles. Part 2: Synthesis and biological evaluation of novel 4,5-dihydro-1H-benzo[g]indazole-based ligands for cannabinoid receptors. (literal)

Abstract

• A series of 4,5-dihydro-1H-benzo[g]indazole-3-carboxamides (2a-k) as analogues of the previously reported CB(2) ligands 6-chloro- and 6-methyl-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamides (1a,b) was synthesized and their affinity and selectivity towards CB(1) and CB(2) receptors were evaluated. Several of the new compounds (2a,b,c,d and i) exhibited CB(1) affinity in the nanomolar range with moderate or negligible affinity towards CB(2) receptors. Compounds 2a and c increased intestinal propulsion in mouse. Their pro-kinetic effects were reversed by the reference CB agonist CP-55,940. Consequently, in vivo CB(1) antagonistic activity was highlighted for these compounds. (literal)

Prodotto di

• Istituto di Ricerca Genetica e Biomedica (IRGB) (Istituto)
• Drug design, drug delivery e valutazione preclinica di nuove entità chimiche. (ME.P06.013.001) (Modulo)

Autore CNR

• LUCA PANI (Unità di personale interno)

Incoming links:

Prodotto

• Istituto di Ricerca Genetica e Biomedica (IRGB) (Istituto)
• Drug design, drug delivery e valutazione preclinica di nuove entità chimiche. (ME.P06.013.001) (Modulo)

Autore CNR di

• LUCA PANI (Unità di personale interno)

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

• Bioorganic & medicinal chemistry (Rivista)