Setembro 2013 vol. 1 num. 1 - Brazilian Meeting on Organic Synthesis 2011

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Docking and Synthesis of a series of 1-(naphthalen-1- ylmethyl)-2-(pyridin-2-yl)-1H-benzo[d]imidazole derivatives designed as novel CB1 cannabinoid ligands.

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

Abstract:

The benzimidazole system has been focus of our attention owing to their affinity to CB2 cannabinoid receptors. However there are few reports of their CB1 receptors affinity. A preliminary screening of our library of benzimidazole derivatives yielded the hit compound C6 (figure1), a potent cannabinoid ligand. This molecule is structurally related to WIN 55212-2, a well know CB1 receptor agonist. In order to generate new CB1 ligands with a benzimidazole framework we made a docking study on a CB1 model, and we identified four possible zones of chemical modification (figure 1). Following this criteria we synthesized a series of 48 molecules which are being currently biologically evaluated (binding assays).

Abstract:

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Palavras-chave: benzimidazoles, cannabinoids, heterocycles,

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DOI: 10.5151/chempro-14bmos-R0233-1

Referências bibliográficas
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Como citar:

Mella-Raipán, J.; Lagos, C. F.; Romero-Parra, ; Espinosa-Bustos, C J.; Pessoa- Mahana, H.; Recabarren-Gajardo, G.; Pessoa-Mahana, C. D.; "Docking and Synthesis of a series of 1-(naphthalen-1- ylmethyl)-2-(pyridin-2-yl)-1H-benzo[d]imidazole derivatives designed as novel CB1 cannabinoid ligands.", p. 233-234 . In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 1, Setembro.2013. São Paulo: Blucher, 2013.
ISSN 2318-4043, DOI 10.5151/chempro-14bmos-R0233-1

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