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555940 
Journal Article 
HPLC-based lipophilicity of pyrrolyl-acetic acid ARIs: Relationships with biological activity 
Chrysanthakopoulos, M; Nicolaou, I; Demopoulos, VJ; Tsantili-Kakoulidou, A 
2010 
Yes 
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences
ISSN: 1570-0232
EISSN: 1873-376X 
878 
1 
61-67 
English 
19948428 
Reversed phase HPLC was used to assess the lipophilicity of a series pyrrolyl-acetic acid derivatives with aldose reductase inhibitory activity. The pH conditions were adjusted at 3.0 to investigate the behavior of the neutral species and at pH 7.4, at which the ionized form predominates, using phosphate and MOPS buffer. Retention was monitored in absence and in presence of different amounts of n-octanol in the mobile phase in order to explore the chromatographic conditions which best reproduce the octanol-water partition or distribution coefficients. The effect of n-octanol in retention was systematically studied and its role in lipophilicity assessment was evaluated. Nevertheless rather moderate regression equations were obtained, which deviated significantly from the ideal 1:1 correlation. No significant effect of buffer was observed. The appropriateness of retention factors to be used in correlation with aldose reductase inhibitory activity was further evaluated and compared to the efficiency of the corresponding octanol-water log P values. 
Pyrrolyl-acetic acid derivatives; Lipophilicity; RP-HPLC; n-Octanol as mobile phase additive; Aldose reductase inhibitory activity 
• Methanol (Non-Cancer)
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