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 (includin...

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Main Authors: Ke Yang, Xinhui Pan
Format: Article
Language:English
Published: MDPI AG 2022-11-01
Series:Medical Sciences Forum
Subjects:
Online Access:https://www.mdpi.com/2673-9992/14/1/128
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author Ke Yang
Xinhui Pan
author_facet Ke Yang
Xinhui Pan
author_sort Ke Yang
collection DOAJ
description 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 <b>3f</b>, <b>3o</b> and <b>3r</b> showed the strongest inhibitory activity (mic of 2–32 μg/mL). Compounds <b>3f</b>, <b>3h</b>, <b>3i</b>, <b>3o</b> and <b>3r</b> 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.
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spelling doaj.art-364455cf7d3c4d7fabeff7b4ffcc8f412023-11-17T12:58:32ZengMDPI AGMedical Sciences Forum2673-99922022-11-0114112810.3390/ECMC2022-13172Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial AgentsKe Yang0Xinhui Pan1Laboratory of Xinjiang Phytomedicine Resource and Utilization, Ministry of Education, School of Pharmaceutical Sciences, Shihezi University, Shihezi 832002, ChinaLaboratory of Xinjiang Phytomedicine Resource and Utilization, Ministry of Education, School of Pharmaceutical Sciences, Shihezi University, Shihezi 832002, ChinaA 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 <b>3f</b>, <b>3o</b> and <b>3r</b> showed the strongest inhibitory activity (mic of 2–32 μg/mL). Compounds <b>3f</b>, <b>3h</b>, <b>3i</b>, <b>3o</b> and <b>3r</b> 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.https://www.mdpi.com/2673-9992/14/1/128synthesisanti-bacterialanti-fungal2-phenylindole
spellingShingle Ke Yang
Xinhui Pan
Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents
Medical Sciences Forum
synthesis
anti-bacterial
anti-fungal
2-phenylindole
title Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents
title_full Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents
title_fullStr Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents
title_full_unstemmed Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents
title_short Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents
title_sort synthesis of novel 2 phenylindole analogues as antifungal and antibacterial agents
topic synthesis
anti-bacterial
anti-fungal
2-phenylindole
url https://www.mdpi.com/2673-9992/14/1/128
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