Synthesis of tacrine-lophine hybrids

Synthesis of tacrine-lophine hybrids

Lopes, João Paulo B.; Costa, Jessé S. da; Russowsky, Dennis; Ceschi, Marco Antonio

Abstract:

Our research group has been involved in the development of cholinesterases (ChEs) inhibitors as potential drugs of Alzheimer’s disease (AD). Tacrine (1) was the first approved ChEs inhibitor by the FDA for the treatment of AD, although its side effects, the search for tacrine hybrids is very important. The bis(7)-tacrine analogues linked by an alkylene chain (bis(n)-cognitin) were prepared and it was proved that these dimeric molecules of tacrine offered a much stronger potency. As part of our studies directed towards the synthesis and biological screening for compounds with ChEs inhibitory activity, we describe herein or studies on the synthesis of a new series of tacrine-lophine hybrids linked by an alkylene chain.

Our research group has been involved in the development of cholinesterases (ChEs) inhibitors as potential drugs of Alzheimer’s disease (AD). Tacrine (1) was the first approved ChEs inhibitor by the FDA for the treatment of AD, although its side effects, the search for tacrine hybrids is very important. The bis(7)-tacrine analogues linked by an alkylene chain (bis(n)-cognitin) were prepared and it was proved that these dimeric molecules of tacrine offered a much stronger potency. As part of our studies directed towards the synthesis and biological screening for compounds with ChEs inhibitory activity, we describe herein or studies on the synthesis of a new series of tacrine-lophine hybrids linked by an alkylene chain.

Palavras-chave:

DOI: 10.5151/chempro-14bmos-R0029-1

Referências bibliográficas

• [1] 1Pisoni, D. S., da Costa, J. S.; Gamba, D.; Petzhold, C. L.; Borges, A. C. A.; Ceschi, M. A.; Lunardi, P.; Gonçalves, C. A. S.; Eur. J. Med. Chem. 2010, 45, 526..
• [2] 2 Kozurkova, M.; Hamulakova, S.; Gazova, Z.; Paulikova, H.; Kristian, P ,Pharmaceuticals 2011, 4, 382.

Como citar:

Lopes, João Paulo B.; Costa, Jessé S. da; Russowsky, Dennis; Ceschi, Marco Antonio; "Synthesis of tacrine-lophine hybrids", p-29-29. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 1, Setembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-14bmos-R0029-1