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Sintesi e valutazione biologica di carbossammidi pirazoliche tricicliche contenenti cicloalchili quali nuovi ligandi cannabinergici

Deiana, Valeria (2014) Sintesi e valutazione biologica di carbossammidi pirazoliche tricicliche contenenti cicloalchili quali nuovi ligandi cannabinergici. Doctoral Thesis.

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Abstract

Cannabinoid receptor ligands are potential candidates for the therapy of chronic pain, neuroinflammatory diseases, cancer and obesity. In preceding studies the relevance and structure-activity relationships (SAR) of pyrazole derivatives have been consolidated and clarified, and in the process three series of tricyclic compounds as 1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazoles, 4,5-dihydro-1H-benzo[g]indazoles and 1,4-dihydroindeno[1,2-c]pyrazoles emerged as potent cannabinoid receptor ligands. In the present study five new series of 1,4-dihydroindeno[1,2-c]pyrazole and 1H-benzo[g]indazole carboxamides containing a cyclopropyl, cyclopentyl or cycloexyl substituent were designed and synthesized to evaluate their affinities towards CB1 and CB2 receptors. Among these derivatives, compound 38Am, exibits a high affinity for CB2 receptor (Ki = 4.48nM) together with remarkable selectivity (KiCB1/KiCB1 = 2232). It is interesting to note, in a in vitro neuroinflammatory test, that compound 3Am shows antagonist activity. Unexpectedly, compound 38Aa possess a agonistic biological profile.

Item Type:Doctoral Thesis
ID Code:9541
Contributors:Pinna, Gérard Aimé
Publisher:Università degli studi di Sassari
Uncontrolled Keywords:Cannabinoidi, pirazoli triciclici
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Cicli, scuole e corsi:Ciclo 26 > Scienze e Tecnologie chimiche > Scienze farmaceutiche
Deposited On:31 Mar 2014 11:17

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