Synthesis of benzyl and phenethylamines as possible nicotinic receptor antagonists

Synthesis of benzyl and phenethylamines as possible nicotinic receptor antagonists

Méndez, Carolina; Pérez, Edwin G.; Cassels, Bruce K.; Caroli, Marcos

Abstract:

Development of selective agonists or antagonists for the Nicotinic acetylcholine receptors (nAChR) may result in new and potentially useful therapeutic agents. It has been reported in the literature that potent and selective nAChR antagonists could be used for the treatment of nicotine dependence and may be an efficacious adjuvant therapy in many different oncologic protocols. nAChr antagonists studied previously by us having an indole ring core, N1-alkyl groups and a quaternized moiety showed potency but little selectivity.

Development of selective agonists or antagonists for the Nicotinic acetylcholine receptors (nAChR) may result in new and potentially useful therapeutic agents. It has been reported in the literature that potent and selective nAChR antagonists could be used for the treatment of nicotine dependence and may be an efficacious adjuvant therapy in many different oncologic protocols. nAChr antagonists studied previously by us having an indole ring core, N1-alkyl groups and a quaternized moiety showed potency but little selectivity.

Palavras-chave:

DOI: 10.5151/chempro-14bmos-R0377-1

Referências bibliográficas

• [1] 1 Dasgupta, p.; Kinkade, R.; Joshi, B.; DeCook, C.; Haura, E.; Chellappan, S. Proc. Natl. Acad. Sci. U.S.A.., 2006, 103, 6332.
• [2] 2 Grozio, A.; Peleari, L.; Catassi, A.; Servent, D.; Cilli, M.; Piccardi, F.; Paganuzzi, M.; Cesario, A.; Granote, P.; Mourier, G.; Russo, P. Int. J. Cancer, 2008, 122, 1911.
• [3] 3 Pérez, E. P.; Eibl, C.; Gundisch, D.; Cassels B. K. Bioorg. Med. Chem. 2011. Acepted.

Como citar:

Méndez, Carolina; Pérez, Edwin G.; Cassels, Bruce K.; Caroli, Marcos; "Synthesis of benzyl and phenethylamines as possible nicotinic receptor antagonists", p-377-377. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 1, Setembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-14bmos-R0377-1