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  • 1 Medical University of Łódź Department of Analytical Chemistry Muszyńskiego 1 90-151 Łódź Poland
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Quantitative structure-activity relationships (QSAR) between H 1 -histaminergic activity and chromatographic data have been investigated for derivatives of 2-[2-(phenylamino)thiazol-4-yl]ethanamine, 2-(2-benzyl-4-thiazolyl)ethanamine, 2-(2-benzhydrylthiazol-4-yl)ethanamine, 2-(1-piperazinyl)benzothiazole, and 2-(hexahydro-1 H -1,4-diazepin-1-yl)benzothiazole. TLC was performed on normal-phase plates (silica gel 60F 254 ) impregnated with solutions of amino acid analogs (propionic acid, propionamide, and n -amylamine) and their mixtures, and with two mobile phases — these systems were selected as models of antagonistic interaction with the human histamine H 1 -receptor. Lipophilicity data were obtained for the compounds examined and used in the QSAR assays. Relationships between chromatographic data and biological activity were found by regression analysis. The correlations obtained in these NP TLC experiments were more significant than those obtained in experiments with RP2 TLC, because of optimum fitting of the chromatographic conditions to the lipophilicity of the solutes. All the chromatographic models proposed should facilitate pre-selection of new drug candidates. Significant correlation ( R 2 = 0.92−0.96) was obtained between p A 2 (H 1 ) values predicted for the compounds by the use of the best equations and the p A 2 (H 1 ) values obtained for the compounds from biological tests.

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Journal of Planar Chromatography - Modern TLC
Language English
Size A4
Year of
Foundation
1988
Volumes
per Year
1
Issues
per Year
6
Founder Akadémiai Kiadó
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Address
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Springer Nature Switzerland AG
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ISSN 0933-4173 (Print)
ISSN 1789-0993 (Online)

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