Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and Triindolylmethanes

Abstract

Methods for the synthesis of hybrid molecules that combine the structure of a highly active antimicrobial compounds - tris(1-alkylindol-3-yl)methylium as well as 3-(indol-1-yl)maleimides that previously showed activity against some protein kinases have been developed. The main purpose of this study was to investigate the influence of substituents on the activity of compounds against different test microorganisms, as well as their toxicity on human cells. For example, with the introduction of a fragment of maleimide, it was possible to reduce cytotoxicity by almost 40 times compared to the original prototype in some cases. At the same time, antimicrobial activity of the new substance remained approximately at the same level.

Keywords

• hybrid antibiotics
• triindolylmethane derivatives
• maleimides
• chemical synthesis
• antibacterial and antifungal activity in vitro
• relations between structure and biological activity