The anticonvulsant, local anesthetic and hemodynamic properties of some chiral aminobutanol derivatives of xanthone.

In the present study, several pharmacological tests in animals were carried out to assess potential anticonvulsant, local anesthetic and hemodynamic activity of novel 2- and 4-substituted aminobutanol chiral derivatives of xanthone (hydrochlorides of: (R,S)-2-[(7-chloro)-2-xanthonemethyl)]-N-methylaminobutan-1-ol (MH-2(R,S)), (R,S)-2-(4-xanthonemethyl)-aminobutan-1-ol (MH-20(R,S)) and (R,S)-2-[(6-methoxy)-2-xanthonemethyl]-aminobutan-1-ol (MH-26(R,S)) and their pure enantiomers R and S). The obtained results provided evidence that the most interesting anticonvulsant (in maximal electroshock-test) activity was shown by compound MH-2(R), which in dose 100 mg/kg p.o.

Anticonvulsant and antidepressant activity of the selected terpene GABA derivatives in experimental tests in mice.

The present study was designed to investigate the central nervous system activity of terpene GABA (and piracetam) derivatives designated as BF-1, BF-2, BF-3, BF-4, BF-5, BF-6. We assessed their anticonvulsant activity in the two main mouse models of seizures (MES-test, PTZ-test), an antidepressant-like effect in the forced swim test (FST), as well as an influence on spontaneous locomotor activity. Our study demonstrated the strong anticonvulsant activity of (1S,3R,7R)-(-)-3,8,8-trimethyl-4-aza-bicyclo[5.

The influence of some aminoalkanolic xanthone derivatives on central nervous and cardiovascular systems in rodents.

A series of appropriate aminoalkanolic derivatives 2- or 4-methylxanthone was synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scPtz) assays, and for neurotoxicity (TOX). The most interesting result was the anticonvulsant activity of (R,S)-2N-(6-chloro-2-xanthonemethyl-2N-methylamino-1-propanol hydrochloride (II, which displayed anti-MES and anti-scPtz activity. Some of the obtained compounds (I - IV and V - VII) were also tested for their effect on the circulatory system (the effect on normal electrocardiogram, protection against adrenaline-, barium-, calcium- and/or strophanthine-induced arrhythmias, the effect on the arterial blood pressure and respiratory movements) and acute toxicity.

New xanthone derivatives as potent anti-inflammatory agents.

Unlabelled: A series of novel xanthone derivatives were synthesized as potential anti-inflammatory compounds. The compounds were examined for anti-inflammatory and analgesic properties. Aspirin and ketoprofen were used as reference compounds.

Influence of new gamma-hydroxybutyric acid amide analogues on the central nervous system activity in mice.

The present study investigates the activity of four gamma-hydroxybutyric acid amide analogues (BM-68, BM-74, BM-75 and BM-76) in two models of chemically induced seizures, i.e. picrotoxin- and pentetrazole-induced seizures and in the thiopental-induced sleep test.