3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase

Abstract

This work presents a study of the several organic compounds such as trihalomethylated enaminones, γ-amino alcohols, oxazinones, oxazines, dihydrofuranones, pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy on the acetylcholinesterase enzyme activity. Also, this work shows the effect per se of organic solvents on the AChE of different cerebral structures of rats. The N- and N-O-alkylated 3-alkoxy-5-hydroxy-trifluormethyl-pyrrolidin-2-ones and trifluoromethylated enoylcarbamates showed in vitro inhibitory effect of the AChE activity in the striatum cerebral of rat, at the concentration 1.0 mM. The dimethyl-[(2-methylsulfanyl-4-trichloromethyl-6-pyrimidin-ylmethoxy)-ethyl] amine showed significant inhibitory effect (p<0.001) in vitro on AChE activity of the striatum cerebral of rat, in the concentration 0.1mM. The in vivo effect of this pyrimidine was significant (p<0.001) in the concentration of 10mg/Kg in the AChE activity in striatum and erythrocyte of rat. Finally, the trifluoromethylated 3-diethoxy-phosphoryloxy ethyl carbamates show significant inhibitory effect (p<0.001) on the purified AChE activity at the concentration of 0.001 mM.