J. Obniska, K. Kamiński
Jun 1, 2005
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Influential Citations
4
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Journal
JPC – Journal of Planar Chromatography – Modern TLC
Abstract
The lipophilicity of twenty-one N-benzyl-2-azaspiro[4.4]nonaneand [4.5]decane-1,3-dione derivatives, fifteen of which (1–15) are active anticonvulsants and six of which (16–21) are inactive, has been determined by reversed-phase thin-layer chromatography with a mixture of n-propanol and TRIS buffer (pH 7.0) as mobile phase. Examination of chromatographic behavior revealed a linear correlation between RM values and the concentration of n-propanol in the mobile phase. The partition coefficients (log P) of the compounds were also calculated by use of the Prolog P module of the Pallas program. Comparison of RM0 and the calculated values of log P for all the derivatives revealed the correlation expressed by the equation RM0 = 0.4882clog P + 0.9488 (r = 0.8964, n = 21). The role of lipophilicity in the anticonvulsant activity of a set of investigated compounds is discussed. The active anticonvulsants were less lipophilic than the inactive compounds.