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.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 52, No. 1, pp. 19 – 28, January, 2018.
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Zhmurenko, L.A., Voronina, T.A., Litvinova, S.A. et al. Synthesis and Anticonvulsive Activity of 3- and 4-Benzoylpyridine Oxime Derivatives. Pharm Chem J 52, 42–51 (2018). https://doi.org/10.1007/s11094-018-1763-z
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DOI: https://doi.org/10.1007/s11094-018-1763-z