Determination of lipophilicity of γ‐butyrolactone derivatives with anticonvulsant and analgesic activity using micellar electrokinetic chromatography. Issue 20 (3rd October 2013)

• Record Type: Journal Article
• Authors: Bajda, Marek; Guła, Aleksandra; Więckowski, Krzysztof; Malawska, Barbara
• Is Part Of: Electrophoresis. Volume 34:Issue 20/21(2013:Oct.)
• Page Start: 3079
• Page End: 3085
• Publication Date: 2013-10-03
• Subjects: Electrophoresis -- Periodicals; Electrophoresis -- Periodicals; 541.372
• DOI: 10.1002/elps.201300266
• Languages: English
• ISSNs: 0173-0835

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>The lipophilicity of a library of 30 derivatives of dihydrofuran‐2(3H)‐one (γ‐butyrolactone) was determined by MEKC. Calibration curve prepared for ten reference drugs enabled to calculate partition coefficient (log <italic>P</italic>) for novel compounds. The results of MEKC analysis were compared with lipophilicity coefficients determined by RP‐TLC (<italic>R</italic>_M0) and computational (Mlog <italic>P</italic>, Clog <italic>P</italic>) methods. Good correlation was observed between the results obtained by both experimental methods: the MEKC parameters log <italic>k</italic> and relative lipophilicity <italic>R</italic>_MO. The relationship between determined log <italic>P</italic> values and results of the computational prediction was weaker. Analysis of the relationship between lipophilicity and anticonvulsant activity showed statistically significant differences between mean values of log <italic>P</italic> coefficients for group of active (2.18) and inactive (1.51) compounds in the maximal electroshock test.</p> </abstract>