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Bioorg Chem. 2011 Aug;39(4):138-42. doi: 10.1016/j.bioorg.2011.05.001. Epub 2011 May 12.

Synthesis and biological activity of derivatives of tetrahydroacridine as acetylcholinesterase inhibitors.

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1
Department Pharmaceutical Chemistry and Drug Analyses, Medical University, ul. Muszyńskiego 1, 90-151 Lodz, Poland. pawel.szymanski@umed.lodz.pl

Abstract

Current state of medical sciences does not allow to treatment neurodegenerative diseases such as Alzheimer's disease (AD). At present treatment of AD is severely restricted. The main class of medicines which are applied in AD is acetylcholinesterase inhibitors (AChEIs) like tacrine, donepezil, galantamine and rivastigmine that do not contribute to significant and long-term improvement in cognitive and behavioural functions. In this work, we report synthesis and biological evaluation of new hybrids of tacrine-6-hydrazinonicotinamide. The synthesis was based on the condensation reaction between tacrine derivatives and the hydrazine nicotinate moiety (HYNIC). All obtained compounds present affinity for both cholinesterases and are characterized by high selectivity in relation to butyrylcholinesterase (BChE).

PMID:
21621811
DOI:
10.1016/j.bioorg.2011.05.001
[Indexed for MEDLINE]
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