Synthesis, brain antihypoxic activity and cell neuroprotection of 1-substituted-3,7-dimethylxanthines

A. Zlatkov, P. Peikov, J. Rodriguez-Alvarez, N. Danchev, I. Nikolova, J. Mitkov

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Abstract

Five newly synthesised original compounds were investigated for cute toxicity, influence on hexobarbital sleeping time, effect on the locomotor activity, and brain antihypoxic activity. Two of the compounds were tested in a model of glutamate induced neurotoxicity in the brain cell culture using a cell viability test. Our studies indicate that compounds 2a-c and 4 prolonged the survival time of mice in the model of anoxic hypoxia. Only compound 3 expressed antihypoxic activity in the model of circulatory hypoxia, evaluated with a statistical significant increase of the survival time. Compound 4 (1-[3-(2,3,dihydro-3-oxobenzisosulfonazol-2-yl)-propyl]-3,7-dimethylxanthine) in concentration range 0.3-3 μM statistically significantly antagonised the gutamate induced neurotoxicity. Compound 4 is important for further investigations on in vivo models of brain dementia. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
Original languageEnglish
Pages (from-to)941-948
JournalEuropean Journal of Medicinal Chemistry
Volume35
DOIs
Publication statusPublished - 1 Jan 2000

Keywords

  • 3,7-dimethyixanthines
  • Acute toxicity
  • Brain antihypoxic activity
  • Glutamate induced neurotoxicity

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