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Synthesis of tacrine-lophine hybrids via one-pot four component reaction and biological evaluation as acetyl- and butyrylcholinesterase inhibitors

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Synthesis of tacrine-lophine hybrids via one-pot four component reaction and biological evaluation as acetyl- and butyrylcholinesterase inhibitors

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Título Synthesis of tacrine-lophine hybrids via one-pot four component reaction and biological evaluation as acetyl- and butyrylcholinesterase inhibitors
Autor Costa, Jesse Sobieski da
Lopes, João Paulo Bizarro
Russowsky, Dennis
Petzhold, Cesar Liberato
Borges, Antônio César de Amorim
Ceschi, Marco Antonio
Konrath, Eduardo Luis
Batassini, Cristiane
Lunardi, Paula Santana
Goncalves, Carlos Alberto Saraiva
Abstract A novel series of tacrine-lophine hybrids was synthesized and tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 in the nanomolar concentration scale. The key step is the one-pot four component condensation reaction of 9-aminoalkylamino-1,2,3,4- tetrahydroacridines, benzil, different substituted aromatic aldehydes and NH4OAc, using InCl3 as the best catalyst. Tacrine-lophine hybrids were found to be potent and selective inhibitors of cholinesterases. As an extension of the four component approach to tetrasubstituted imidazoles, a new series of bis-(2,4,5- triphenyl-1H-imidazoles) or bis(n)-lophines was tested against AChE and BuChE.
Contido em European journal of medicinal chemistry. Paris. Vol. 62, (Apr. 2013), p. 556-563
Assunto Sintese organica
Tacrina
[en] AChE inhibitory activity
[en] Four component reaction
[en] Indium trichloride
[en] Lophine
[en] Tacrine
Origem Estrangeiro
Tipo Artigo de periódico
URI http://hdl.handle.net/10183/83620
Arquivos Descrição Formato
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