New Biologically Active Compounds in the Series of 3-(indol-1-yl)-, 3-(N-aminoaryl)-, and 3-(S-thioaryl)Maleimide Derivatives

Abstract

Novel compounds among 3,4-disubstituted maleimlde derivatives that reveal a pronounced antimicrobial activity in vitro against Gram-positive bacteria, yeast Candida albicans, and fungi Aspergillus niger were obtained through total chemical synthesis. All these derivatives were simultaneously inactive against Gram-negative bacteria Escherichia coli, indicating the specific nature of their antimicrobial action. A number of derivatives appeared to be active in Halobacterium salinarum test system, which is used for selecting biologically active compounds among sterol biosynthesis inhibitors and antitumor antibiotics. This data suggests that such derivatives seem to have potential antitumor properties. The most active compounds were 3-bromo-4-thioaryl and 3,4-bisthioaryl maleimides, which are related to a new type of chemical compounds, that are promising for further elaboration and development of new antimicrobial and antitumordrugs on their basis.

Keywords

• maleimides
• indolylmaleimides
• thioarylmaleimides
• trisalkylindolylmethan derivatives
• antimicrobial and antitumor compounds
• antibacterial and antifungal activity in vitro
• halobacterium salinarum microbial model in screening of antibiotics