THE ACUTE TOXICITY AND ANALGESIC ACTIVITY INVESTIGATION OF NEW SPIROCYCLIC PYRAZOLIDINE-3,5-DIONE DERIVATIVES

V. M. Holovatiuk, O. A. Brazhko, V. I. Kashkovsky

Abstract


We presented the results of acute toxicity and analgesic activity research of the new spirocyclic pyrazolidine-3,5-dione derivatives. We studied the acute toxicity of spirodiazolidines with QSAR analysis by QuS computer design and experimentally on mammalian (mice). These compounds had low toxicity and toxic values that decreased with introduction of methyl substituent in cyclopentenic ring and other substituents in compound aromatic fragments. The acute toxicity values that were obtained by nonexperimental and experimental methods had similar magnitudes, and this will allow to apply the computer prognosis in further investigations and design of new bioactive molecules. We also carried out the research of analgesic activity of new spirocyclic pyrazolidinedione derivatives. We proved that some compounds of the studied range have significant analgesic activity to be competed with well-known pyrazolone containing drug ‘Analgin’.


Keywords


pyrazolidinedione; acute toxicity; analgesic activity

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DOI: http://dx.doi.org/10.15421/201681

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