Acta Pharm. 57 (2007) 361-370

10.2478/v10007-007-0029-1
 

full paper

Short communication

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

JAVOR MITKOV¹, NIKOLAI DANCHEV², IRINA NIKOLOVA² and ALEXANDER ZLATKOV^1*

alexbz2000@yahoo.com

¹ Department of Pharmaceutical Chemistry, Faculty of Pharmacy, 1000 Sofia, Bulgaria

² Department of Pharmacology and Toxicology, Faculty of Pharmacy, 1000 Sofia, Bulgaria

Accepted April 27, 2007

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

Keywords: caffeine-8-thioglycolic acid, aliphatic and arylaliphatic amides, brain antihypoxic activity, acute toxicity