Action of Some Synthetic Choleretic Compounds in Chronic Biliary Fistula Dogs

Abstract
Some of the synthetic choleretic compounds found to be potent in acute biliary fistula dogs were further investigated in chronic biliary fistula dogs. The potency of these compounds on bile secretion in a daily dose of 0.5 g. was compared with that of Ketochol in a daily dose of 1.5 g. The order of potency was as follows: -l-bromo-2-hydroxy-3-naphthoic acid (SC 2156); beta-(2,4-dimethoxy-5-cyclopentylmethylbenzoyl)-propionic acid (SC 2798); beta_(2,4-dimethoxy-5-cyclohexylbenzoyl)- propionic acid (SC 2644); beta-(2,4-dimethoxy-5-benzylbenzoyl)-propionic acid (SC 2657); beta-(l-methoxy-4-naphthoyl)-propionic acid (SC 1749); mixture of ketocholanic acids, chiefly dehydro-cholic acid (Ketochol); 2,4-diacetyl-1-naphthol (SC 2224); beta-(2-methoxy-5-cyclohexylbenzoyl)-propionic acid (SC 2292); podocarpic acid (SC 1852); beta-(5-acenaphthyl)_acrylic acid (SC 2061); beta-(5-acenaphthoyl)-acrylic acid (SC 1643); 6-carboxy-methoxy-l,12-dimethyl-1,2,3,4,9,10,12-octahydrophenanthrene-l.carboxylic acid (SC 1977); gamma-oxo-gamma-(3 phenoxthin)-butyric acid (SC 1834); gamma-oxo-gamma_(2 hydroxydiphenyl_5-)-butyric acid (SC 1745); beta-(3-cyclohexyl-4_hydroxybenzoyl)-propionic acid (SC 2230); beta-(5,6,7,8-tetrahydro_2-hydroxy-l-naphthoyl)-propionic acid (SC 2136); beta-(1-methoxy-4-naphthoyl)-acrylic acid (SC 2226); beta-(1-hydroxy-4-naphthoyl)-propionic acid (SC 1561); beta-(2-hydroxy-4-methoxy)-benzoyl propionic acid (SC 1683); gamma-oxo-gamma-(2 phenoxthin)-butyric acid (SC 1881); and trithioparamethoxyphenyl-dithia-4,5-cyclopentene-2-thione-1 (SC 2438). SC 2156 and SC 2644 manifested some toxic effect. All of these compounds were admd. orally, therefore, low potencies might have been due to poor absorption from the intestine. The structure-activity relationship of the potent compounds is discussed.
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