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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MDPI AG
2022-11-01
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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. |
first_indexed | 2024-03-11T06:05:58Z |
format | Article |
id | doaj.art-364455cf7d3c4d7fabeff7b4ffcc8f41 |
institution | Directory Open Access Journal |
issn | 2673-9992 |
language | English |
last_indexed | 2024-03-11T06:05:58Z |
publishDate | 2022-11-01 |
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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 |
work_keys_str_mv | AT keyang synthesisofnovel2phenylindoleanaloguesasantifungalandantibacterialagents AT xinhuipan synthesisofnovel2phenylindoleanaloguesasantifungalandantibacterialagents |