Antimicrobial properties of some 3-acyl-4,7-disubstituted indoles.

In continuation of research on indole derivatives as potential chemotherapeutic agents, the antimicrobial properties of some 4,7-disubstituted 3-acylindoles were studied; the derivatives tested were 4,7-dimethoxy-, 4-hydroxy-7-methoxy-, 4,7-dihydroxyindoles and indole 4,7-quinones. Only the dihydroxy compounds (V a-c) proved active against certain bacterial strains. In order to test whether the action mechanism was analogous to that of mitomycin, a series of experiments was carried out to study the formation of complexes with DNA. It was found that only the substances with antimicrobial activity can form complexes, and it is therefore suggested that the action mechanism involves interference with cellular DNA.