1240996-83-1Relevant articles and documents
Tricyclic pyrazoles. Part 6. Benzofuro[3,2-c]pyrazole: A versatile architecture for CB2 selective ligands
Pinna, Giovanni,Loriga, Giovanni,Lazzari, Paolo,Ruiu, Stefania,Falzoi, Matteo,Frau, Simona,Pau, Amedeo,Murineddu, Gabriele,Asproni, Battistina,Pinna, Gerard A.
, p. 281 - 292 (2014/06/24)
A new series of 1H-benzofuro[3,2-c]pyrazole-3-carboxamides was synthesized. The novel compounds (15-24) were evaluated for their affinity to CB2 and CB1 cannabinoid receptors. The synthesis of the title compounds takes advantage of the acid-catalysed thermal cyclization of bicyclic hydrazone ethyl 2-(2-(2,4-dichlorophenyl)hydrazono)-2-(6-methyl-3-oxo-2,3- dihydrobenzofuran-2-yl)acetate to tricyclic ethyl 1-(2,4-dichlorophenyl)-6- methyl-1H-benzofuro[3,2-c]pyrazol-3-carboxylate. All the obtained derivatives showed high affinity to CB2 receptors. Moreover, significant selectivity for CB2 over CB1 receptors was highlighted for lead derivatives amongst the novel series. The best binding profiles were determined for homologues bearing monocyclic and bicyclic monoterpenic substituents at the carbamoyl group at 3 position of the pyrazole ring (K iCB2 2 receptors with Ki values of 3.7 and 2398 nM for CB2 and CB1 receptors, respectively. Preliminary functional assays evidenced CB2 agonism behaviour for all the assayed novel derivatives.
Tricyclic pyrazole derivatives and microemulsions thereof as CB1- and/or CB2-inhibitors
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Page/Page column 57; 58, (2010/09/17)
Microemulsions of pharmaceutical compositions comprising the following components (% by weight), the sum of the components being 100%: S) from 0.01 to 95% of one or more compounds selected from surfactants, polymers forming organized structures as: aggreg
Tricyclic condensed pyrazole derivatives as CB1 inhibitors
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Page/Page column 52; 53, (2010/09/17)
Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring rcomprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous sy