Abstract
Malononitrile, cyanoacetic-acid-methyl- and ethyl-ester, cyanoacetamide, cyanoacetic-acid-hydrazid, cyanoacetanilide and -4-chlor-anilide, acetylaceton, aceto-acetic-ester, malonic-acid-diethylester were coupled with aryl-diazonium salts in the presence of sodium-acetate and their in-vitro bacteriostatic, fungistatic, tuberculostatic, trichomonastatic and ascarizid effects were measured as well as their acute toxicity in rats. It was concluded that only the aryl-azo-malononitriles possess marked biological activity which seems to be related to the structure R-NN-CH(CN) 2 or to its tautomeric form R-NH-NC(CN) 2. The bacteriostatic and fungistatic effect of aryl-azo-malonontriles are considerably decreased by cysteine and thioglycolate (or even inhibited by some of them), but are not influenced by ascorbic acid. The aryl-azo-malononitriles appear to exert their antimicrobial effect by reacting with the sulfhydryl-groups of certain sulfhydryl enzymes—which play an important part in the metabolism of micro-organisms—in a similar manner as with the cystein or thioglycolate. The aryl-azo-malononitriles are a new-type sulfhydryl-enzyme inhibitors of high biological activity and showing a high degree of structural specificity.
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