<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml"><p>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 <sup>1</sup>H NMR data. Values of acute <italic>p.o.</italic> and <italic>i.p.</italic> 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 compounds exhibited brain antihypoxic activity (<bold>5a</bold> and <bold>5b</bold> against haemic and circulatory hypoxia, respectively).</p></abstract>

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 compounds exhibited brain antihypoxic activity (5a and 5b against haemic and circulatory hypoxia, respectively).

Synthesis and brain antihypoxic activity of some aliphatic and arylaliphatic amides of caffeine-8-thioglycolic acid

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, 1000 Sofia, Bulgaria

Department of Pharmacology and Toxicology, Faculty of Pharmacy, 1000 Sofia, Bulgaria

Acta Pharmaceutica

The synthesis of some aliphatic and arylaliphatic amides of caffeine-8-thioglycolic acid was studied. The structures of synthesized compounds were proved by...

Synthesis and brain antihypoxic activity of some aliphatic and arylaliphatic amides of caffeine-8-thioglycolic acid

Publié en ligne: 18 sept. 2007

Pages: 361 - 370

DOI: https://doi.org/10.2478/v10007-007-0029-1

Mots clés
kofein-8-tioglikolna kiselina, alifatski i arilalifatski amidi, antihipoksično djelovanje u mozgu, akutna toksičnost

This content is open access.

Synthesis and brain antihypoxic activity of some aliphatic and arylaliphatic amides of caffeine-8-thioglycolic acid

Publié en ligne: 18 sept. 2007

Pages: 361 - 370

DOI: https://doi.org/10.2478/v10007-007-0029-1

Mots cléskofein-8-tioglikolna kiselina, alifatski i arilalifatski amidi, antihipoksično djelovanje u mozgu, akutna toksičnost

This content is open access.

Mots clés
kofein-8-tioglikolna kiselina, alifatski i arilalifatski amidi, antihipoksično djelovanje u mozgu, akutna toksičnost