Synthesis and Biological Evaluation of NO-Donor-Tacrine Hybrids as Hepatoprotective Anti-Alzheimer Drug Candidates
Journal of Medicinal Chemistry2008Vol. 51(4), pp. 713–716
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Lei Fang, Dorothea Appenroth, Michael Decker, Michael Kiehntopf, Carolin Roegler, Thomas Deufel, Christian Fleck, Sixun Peng, Yihua Zhang, Jochen Lehmann
Abstract
In search of safer anti-Alzheimer drugs, 14 NO-donor-tacrine hybrids (1- 14) were synthesized and evaluated for their ability to inhibit cholinesterases and for vasorelaxation effects. Compounds 1- 13 showed good cholinesterases inhibitory activities in vitro, while 14, particularly, was highly selective, preferring butyrylcholinesterase rather than acetylcholinesterase. Four selected compounds (1, 9, 11, and 14) moderately relaxed the porcine pulmonary arteries in organ bath. In the hepatotoxicity study, significant hepatotoxicity was caused by tacrine but not by 9.
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