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Estimating the lipophilicity of a number of 2‐amino‐1‐cyclohexanol derivatives exhibiting anticonvulsant activity
Authors:
El?bieta P?kala
Henryk Marona
Institution:
Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, 30‐688 Cracow, Poland
Abstract:
The lipophilicity of a number of
N
‐acyl derivatives of
trans
‐ or
cis
‐: racemic, (1
R
,2
R
)‐ or (1
S
,2
S
)‐aminocyclohexanol (1–13) exhibiting anticonvulsant activity was investigated. Their lipophilicity (
R
m 0
) was determined using reversed‐phase thin‐layer chromatography (RP‐TLC) with mixtures of methanol and water as mobile phases. The partition coefficients of compounds 1–13 (log
P
) were also calculated using two computer programs (Pallas and Chem DU) and compared with
R
m 0
. Copyright © 2009 John Wiley & Sons, Ltd.
Keywords:
2‐amino‐1‐cyclohexanol
reversed‐phase thin‐layer chromatography
lipophilicity
retention parameter Rm0
calculated partition coefficient log P
anticonvulsant activity
quantitative structure–
activity relationship
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