Synthesis and cholinesterase inhibitory activity of 6-, 7-methoxy-(and hydroxy-) tacrine derivatives.
Some 6- and 7-methoxy-(and hydroxy-) tacrine derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities. The most potent analogue in our series was the 9-heptylamino-6-methoxytacrine 3af which, in comparison with tacrine (THA), displayed an almost identical inhibitory effect, slightly lower acute toxicity and higher selectivity profile towards AchE when compared with THA.
Del Giudice
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MR
Laboratorio di Chimica del Farmaco, Istituto Superiore di Sanità, Roma, Italy.
Borioni
A
A
Mustazza
C
C
Gatta
F
F
Meneguz
A
A
Volpe
M T
MT
D000818:Animals; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013619:Tacrine / Q000031:analogs & derivatives*
D002800:Cholinesterase Inhibitors; D013619:Tacrine