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Lipophilicity characterization of new N ‐phenylamino‐azaspiranes as potential anticonvulsant agents
Author(s) -
Obniska Jolanta,
Kamiński Krzysztof
Publication year - 2006
Publication title -
biomedical chromatography
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.4
H-Index - 65
eISSN - 1099-0801
pISSN - 0269-3879
DOI - 10.1002/bmc.682
Subject(s) - lipophilicity , chemistry , anticonvulsant , chromatography , characterization (materials science) , pharmacology , stereochemistry , nanotechnology , epilepsy , neuroscience , medicine , materials science , biology
The lipophilicity of a library of N ‐phenylamino‐2‐azaspiro[4.4]nonane‐ and [4.5]decane‐1,3‐dione derivatives has been determined by reversed‐phase thin‐layer chromatography with n ‐propanol–Tris buffer (pH 7.4) mixtures as mobile phases. Examination of chromatographic behaviour revealed a linear correlation between R M values and the concentration of n ‐propanol in the mobile phase. The partition coefficients (log P ) were also calculated by use of the Prolog P module of the Pallas computer program. Comparison of R M0 values and calculated (log P PALLAS ) data revealed the correlation expressed by the equation: log P PALLAS = 0.9995 R M0 + 1.3451 ( n = 28; r = 0.8971; F = 107.13; p < 0.05). The role of the lipophilicity in the anticonvulsant activity of a set of compounds examined is discussed: the active anticonvulsants were less lipophilic than inactive ones. Copyright © 2006 John Wiley & Sons, Ltd.