Synthesis and docking of new benzimidazole derivates designed as novel and potent CB1 cannabinoid ligands.

Synthesis and docking of new benzimidazole derivates designed as novel and potent CB1 cannabinoid ligands.

J., Romero-Parra; C.F., Lagos; C., Espinosa-Bustos; J, Mella-Raipán; Pessoa-Mahana.; G., Recabarren; D., Pessoa-Mahana C.

Abstract:

Despite the fact that medicinal and cognitive effects of Marijuana (Cannabis sativa) have been known for thousands of years, only recent studies provided convincing information on the biological mediation of it effects. Currently, two subtypes of cannabinoid receptor (namely CB1 and CB2) have been cloned and pharmacologically characterized. Both CB1 and CB2 belong to the G protein-coupled receptor family (GPCRs). Knowledge of the characteristics of CB1 binding site has notably increased the interest on the synthesis of new small molecules as potential ligands, significantly less lipophilic and more potent than Δ9- THC2. Our interest in developing new cannabinoid ligands is based on the therapeutic opportunities associated to these chemical entities.

Despite the fact that medicinal and cognitive effects of Marijuana (Cannabis sativa) have been known for thousands of years, only recent studies provided convincing information on the biological mediation of it effects. Currently, two subtypes of cannabinoid receptor (namely CB1 and CB2) have been cloned and pharmacologically characterized. Both CB1 and CB2 belong to the G protein-coupled receptor family (GPCRs). Knowledge of the characteristics of CB1 binding site has notably increased the interest on the synthesis of new small molecules as potential ligands, significantly less lipophilic and more potent than Δ9- THC2. Our interest in developing new cannabinoid ligands is based on the therapeutic opportunities associated to these chemical entities.

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DOI: 10.5151/chempro-14bmos-R0171-1

Referências bibliográficas

• [1] B. Bosier, Giulio G. Muccioli, E.Hermans, D. M. Lambert. Biochemical Pharmacology 2010, 80, 1–12.
• [2] Pál Pacher, Sándor Bátkai, and George Kunos. Rev Article. Pharmacol Rev. 2006, 58, 389-462.

Como citar:

J., Romero-Parra; C.F., Lagos; C., Espinosa-Bustos; J, Mella-Raipán; Pessoa-Mahana., ; G., Recabarren; D., Pessoa-Mahana C.; "Synthesis and docking of new benzimidazole derivates designed as novel and potent CB1 cannabinoid ligands.", p-171-171. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 1, Setembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-14bmos-R0171-1