Mercury diuretic preparations

Diuretic drug preparations have promoted urine formation. They are derivatives of mercury propanol RCH2CH(OH)CH2HgX, where R is a polar hydrophilic group. The mercury diuretic preparations act as ferment inhibitors (latter containing-. They also inhibit adenosine triphosphate (ATP). These properties led to the use of mercury drug compounds in the treatment of bacterial infections. In these cases, they interacted with -SH groups of the bacteria proteins. 

Amino- and hydrazino-quinazolines exhibited antibacterial activity and a patent claim on the in vitro action of 2,4-diamino-quinazolines was made. " The preparation of thiopegan derivatives as potential antimalarials and antibacterials deserves mention. Complete inhibition of influenza virus in vitro but not in vivo was shown by, 6,8-dichloro-2,4-dihydroxyquinazoline and other cyclic ureas. Activity against trachoma virus was also displayed by several 2-trichloromethylquinazolines. 7-Chloro-6-sulfonamido-4(37I)quinazolinones are more effective than the mercury diuretics and can be administered orally. The 1 -dihydro derivatives are even more effective and one (59) has been marketed under the name Quinethazone. ... 

Galen, a physician whose views outUved him by about a thousand years, died about 200 AD. He beUeved that mercurials were toxic, and did not use any mercury compound therapeutically. However, as a result of Arabian influence, the therapeutic uses of mercury were slowly recognized by Western Europe. In the thirteenth century mercury ointments were prescribed for treating chronic diseases of the skin. Mercury and its compounds, such as mercurous chloride, mercuric oxide, mercuric chloride, and mercuric sulfide, were used widely from the fifteenth to the nineteenth centuries, and to some extent in the twentieth century. During the first half of the twentieth century, the primary therapeutic uses of mercury included bactericidal preparations, such as mercuric chloride, mercuric oxycyanide, and mercuric oxide and diuretics, such as aryl HgX (Novasural) and mercurated ahyl derivatives (14). 

The cyclized analog of meralluride is prepared by a similar synthesis. Thus, condensation of camphoric acid (42) (obtained by oxidation of camphor) with ammonia gives the bicyclic succinimide (44). Reaction with allyl isocyanate followed by ring opening and then reaction with mercuric acetate affords the mercury derivative (45) as the acetate rather than the hydroxide as above. Reaction with sodium chloride converts that acetate to the halide (46). Displacement on mercury with the disodium salt of thioglycollic acid affords the diuretic mercaptomerine (47). ... 

This indoline derivative has antihypertensive and diuretic actions. Indapamide (233) in methanol under nitrogen was irradiated with a medium-pressure mercury lamp through a copper sulphate filter solution for 12 h. The filter removed wavelengths below 300 nm. Products were separated by preparative TLC and identified as 2-methylindoline (234), the formylhydrazide (235), the amide (237) and semicarbazide. The procedure was repeated under oxygen to give the above products plus the urethane (236), acid (238), ester (239) and TV-acetylanthranilic acid [146]. 

Mercurials are supposed directly to promote the secretion of bile, or its flow into the intestines. They increase the effect of diuretics and diaphoretics. The following are the principal preparations and their doses ... 

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