Synthesis and Brain Antihypoxic Activity of Some Aminoalcoholic Derivatives of Caffeine-8-thioglycolic Acid
نویسندگان
چکیده
The synthesis and pharmacological activity of some aminoalcoholic derivatives of 8-caffeinethioglycolic acid was studied. The structure of the synthesized compounds was proved by microanalysis, IRand H-NMR spectra. All of the investigated compounds were found to be practically non-toxic (LD50 p.o. > 5 g kg in mice) and less toxic compared to caffeine. The compounds were investigated for antihypoxic activity in three models of experimental hypoxia – asphyctic, haemic and circulatory. Antihypoxic activity was especially pronounced in the model of asphyctic hypoxia. Compound 5a (N,N-Bis-(2-hydroxyethyl)-2(1,3,7-trimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl-sulfanyl)-acetamide) shows the highest activity.
منابع مشابه
Synthesis and brain antihypoxic activity of some aliphatic and arylaliphatic amides of caffeine-8-thioglycolic acid.
The synthesis of some aliphatic and arylaliphatic amides of caffeine-8-thioglycolic acid was studied. The structures of synthesized compounds were proved by micro-analyses, IR- and 1H NMR data. Values of acute p.o. and i.p. toxicity in mice show lower toxicity compared to caffeine. Declines in spontaneous locomotor activity support the idea of depressive CNS activity of the compounds. Two compo...
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