Synthesis and Anticonvulsive Activity of 3- and 4-Benzoylpyridine Oxime Derivatives

Autor:	I. O. Gaidukov, T. A. Gudasheva, S. A. Litvinova, L. A. Zhmurenko, G. V. Mokrov, T. A. Voronina, L. N. Nerobkova
Rok vydání:	2018
Předmět:	Pharmacology Low toxicity medicine.medical_treatment Oxime 01 natural sciences Oxalate 0104 chemical sciences 4-benzoylpyridine 010404 medicinal & biomolecular chemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Therapeutic index Anticonvulsant chemistry Active compound Drug Discovery medicine Antagonism 030217 neurology & neurosurgery
Zdroj:	Pharmaceutical Chemistry Journal. 52:42-51
ISSN:	1573-9031 0091-150X
Popis:	We present here the synthesis of 3- and 4-benzoylpyridine oxime derivatives with potential anticonvulsant action. The most active compound in the maximum electric shock test was 4-benzoylpyridine O-2-morpholinoethyloxime oxalate (1a), i.p. doses of 60 – 150 mg/kg of which increased the survival of mice to 100%. The best effect in the corasol antagonism test was obtained with 4-benzoylpyridine O-(isonicotinoyl)oxime (2c), i.p. doses of 12.5 mg/kg of which increased the survival of mice to 67% and the latent period of onset of generalized tonic-clonic convulsions to 52 sec. Compound 1a had low toxicity (the i.p. LD50 in mice was 316 mg/kg) and a therapeutic index of 21.
Databáze:	OpenAIRE
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