Pharmacological properties of some aminoalkanolic derivatives of xanthone.
A series of appropriate aminoisopropanoloxy derivatives of 2-, 3- or 6-xanthone was synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (ScMet) assays and for neurotoxicity (TOX). The most interesting result was the anticonvulsant activity of (+/-)-3-(2-propylamino)-1- [(2-methyl)-6-xanthonoxy]-2-propanol hydrochloride (10), which displayed anti-MES activity with a protective index (TD50/ED50) of 0.80. Some of the obtained compounds were also tested for their effect on the circulatory system (influence on the non-working heart perfusion, protection against adrenaline induced-arrhythmia) and acute toxicity.
Marona
H
H
Department of Chemical Technology of Drugs, Jagiellonian University, Kraków, Poland.
Pekala
E
E
Filipek
B
B
Maciag
D
D
Szneler
E
E
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D001145:Arrhythmias, Cardiac / Q000139:chemically induced / Q000517:prevention & control; D003326:Coronary Circulation / Q000187:drug effects; D004597:Electroshock; D004837:Epinephrine / Q000494:pharmacology; D006439:Hemodynamics / Q000187:drug effects; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D012640:Seizures / Q000517:prevention & control; D014970:Xanthines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity
D000889:Anti-Arrhythmia Agents; D000927:Anticonvulsants; D014970:Xanthines; D004837:Epinephrine