Studies on structure-diuretic activity relationships of organic compounds of mercury.

According to Friedman ( 1 ), the nature of the X substituent (usually halogen, theophylline or thioglycolate) has no effect on diuretic potency if the compound is given intravenously, but does influence both hyperacute (cardiac and respiratory arrest) and acute (7 to 14-day) renal toxicity. The nature of the OY group is determined by the solvent in which the mercuration is carried out and is an hydroxyl group, if the solvent is water. or a methoxy or ethoxy group, if the solvent is the corresponding alcohol. Within these limits, i.e., OH, OCH3, or OC.,H5, the nature of the OY group is without appreciable effect on either diuretic potency or toxicity. In contrast, the nature of the R group, which is commonly rather complex, has a very great effect on both toxicity and diuretic activity. In the diuretic mersalyl, R is o-carbamylphenoxyacetic acid; in mercaptomerin, R is camphoramic acid; in meralluride, R is succinyl-urea; in chlormerodrin, R is urea; and in mercumatilin, R is coumarin. Much of the interest in the structure-activity relationships of mercurial compounds has centered around the effects of modification of R and relatively less attention has been paid to simple organo-mercurial compounds. A wide variety of substituted allyl compounds