Synthesis of novel 2-phenylindole analogues as antifungal and antibacterial agents

A series of novel indole derivatives containing ester groups, halogen, epoxy and short-chain aliphatic hydrocarbons were designed, synthesized and evaluated for their antibacterial activities. Most of the compounds showed relatively excellent inhibitory activities against different strains (including a multidrug-resistant clinical isolate). Compounds 1f, 1o and 1r showed the strongest inhibitory activity (mic of 2-32 μg/ml). Compounds 1f, 1h, 1i, 1o and 1r with antibacterial activity were not cytotoxic against RAW 264.7 mouse macrophages. Structure-activity relationship analysis and docking studies showed that halogens as well as aliphatic hydrocarbons could enhance the antibacterial ability and reduce the toxicity of the indole compounds