Abstract
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...
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