Synthesis and Anticonvulsive Activity of 3- and 4-Benzoylpyridine Oxime Derivatives
- Authors: Zhmurenko L.A.1, Voronina T.A.1, Litvinova S.A.1, Nerobkova L.N.1, Gaidukov I.O.1, Mokrov G.V.1, Gudasheva T.A.1
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Affiliations:
- V. V. Zakusov Science Research Institute of Pharmacology
- Issue: Vol 52, No 1 (2018)
- Pages: 42-51
- Section: Article
- URL: https://journals.rcsi.science/0091-150X/article/view/244982
- DOI: https://doi.org/10.1007/s11094-018-1763-z
- ID: 244982
Cite item
Abstract
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.
About the authors
L. A. Zhmurenko
V. V. Zakusov Science Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiicheskaya Street, Moscow, 125315
T. A. Voronina
V. V. Zakusov Science Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiicheskaya Street, Moscow, 125315
S. A. Litvinova
V. V. Zakusov Science Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiicheskaya Street, Moscow, 125315
L. N. Nerobkova
V. V. Zakusov Science Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiicheskaya Street, Moscow, 125315
I. O. Gaidukov
V. V. Zakusov Science Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiicheskaya Street, Moscow, 125315
G. V. Mokrov
V. V. Zakusov Science Research Institute of Pharmacology
Author for correspondence.
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiicheskaya Street, Moscow, 125315
T. A. Gudasheva
V. V. Zakusov Science Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiicheskaya Street, Moscow, 125315