Studies on Cardiac Ingredients of Plants. V. : Chemical Transformation of Proscillaridin and Biological Activities of Derivaties

概要

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In order to investigate the relationship between the chemical structures and the biological activities of proscillaridin (1) and related compounds, transformations of the lactone (1) into the lactams (2a-i) with monoalkylamines, into 1,4-cycloadducts (3,5) with dimethyl acetylenedicarboxylate, and into epoxides (6-8) with tris(acetylacetonate)iron(III)-H_2O_2 have been under-taken. Further, alkoxyalkylation of the teriary C_<14β>-hydroxy group was carried out with alkoxyalkyl halides. The biological activities of the resulting proscillaridin derivatives were studied by the use of isolated guinea-pig papillary muscle preparations and an Na^+, K^+-adenosine triphosphatase preparation from dog kidney.Although the activities of proscillaridin derivatives were less potent than that of 1,compounds 2a, 2g, 3 and 9 showed slightly expanded concentration ranges of positive inotropic effect development on guinea-pig papillary muscle preparations.A significant correlation was obtained between the van der Waals volumes (V_w) and pIC_<50> values of 1 and 2a-h (r=-0.09,p<0.01).
社団法人日本薬学会の論文
1988-01-25