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 compounds exhibited brain antihypoxic activity (5a and 5b against haemic and circulatory hypoxia, respectively).
Mitkov
Javor
J
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, 1000 Sofia, Bulgaria.
Danchev
Nikolai
N
Nikolova
Irina
I
Zlatkov
Alexander
A
D000284:Administration, Oral; D000818:Animals; D002110:Caffeine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020925:Hypoxia-Ischemia, Brain / Q000188:drug therapy / Q000517:prevention & control*; D007274:Injections, Intraperitoneal; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D013864:Thioglycolates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D023382:Toxicity Tests, Acute / Q000379:methods
D013864:Thioglycolates; D002110:Caffeine