Abstract
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 3f, 3o and 3r showed the strongest inhibitory activity (mic of 2–32 μg/mL). Compounds 3f, 3h, 3i, 3o and 3r with antibacterial activity were not cytotoxic against RAW 264.7 mouse macrophages. The structure–activity relationship analysis and docking studies showed that the halogens as well as aliphatic hydrocarbons could enhance the antibacterial ability and reduce the toxicity of the indole compounds.
Supplementary Materials
The following are available online at https://www.mdpi.com/article/10.3390/ECMC2022-13172/s1.
Author Contributions
Conceptualization, X.P.; methodology, X.P.; experiment, K.Y., software, K.Y.; validation, X.P.; formal analysis, K.Y.; investigation, K.Y.; resources, K.Y.; data curation, K.Y.; writing—original draft preparation, K.Y.; writing—review and editing, X.P.; supervision, X.P. All authors have read and agreed to the published version of the manuscript.
Funding
This study was supported by National Natural Science Foundation of China (82160651); The Open Project of Stake Key Laboratory of Natural and Biomimetic Drugs, Peking University (K202103); The Open Project of Key Laboratory of Xinjiang Phytomedicine Resource and Utilization, Ministry of Education (XPRU202004); Youth Innovative Talent Cultivation Projects of Shihezi University (CXPY202005) and The Open Sharing Fund for the Large-scale Instruments and Equipments of Shihezi University.
Institutional Review Board Statement
The animal study protocol was approved by the Ethics Committee of the First Affiliated Hospital, School of Medicine, Shihezi University (protocol code A2022-209-01).
Informed Consent Statement
Not applicable.
Data Availability Statement
The data presented in this study are available in the article.
Conflicts of Interest
The authors declare no conflict of interest.
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