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Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria

Quorum sensing is a well-known term for describing bacterial cell–cell communication. Bacteria use quorum sensing pathways to respond to external factors such as nutrient availability, defense mechanisms, and coordinate host toxic behaviors such as biofilm formation, virulence production, and other...

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Main Authors: Tung Truong Thanh, Huy Luong Xuan, Thang Nguyen Quoc
Format: Bài trích
Language:eng
Published: RSC advances 2021
Online Access:https://pubs.rsc.org/en/content/articlelanding/2021/RA/D1RA03616E
https://dlib.phenikaa-uni.edu.vn/handle/PNK/2865
https://doi.org/10.1039/D1RA03616E
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spelling oai:localhost:PNK-28652022-08-17T05:54:49Z Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria Tung Truong Thanh Huy Luong Xuan Thang Nguyen Quoc Quorum sensing is a well-known term for describing bacterial cell–cell communication. Bacteria use quorum sensing pathways to respond to external factors such as nutrient availability, defense mechanisms, and coordinate host toxic behaviors such as biofilm formation, virulence production, and other pathogenesis. Discovery of novel compounds which inhibit quorum sensing without being antibiotic are currently emerging fields. Herein, the library of fifteen benzo[d]thiazole/quinoline-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl compounds was designed, synthesized and evaluated to find novel quorum sensing inhibitors. Firstly, compounds were evaluated for their growth inhibitory activities at high concentrations up to 1000 μg mL−1 toward Pseudomonas aeruginosa. Under our conditions, twelve compounds showed moderate growth inhibitory activities in the concentration tested. To our delight, three compounds 3, 6 and 7 do not affect the growth of the bacteria which were chosen for the evaluation of quorum sensing inhibitor activities. In the LasB system, our compounds 3, 6, 7 showed promising quorum-sensing inhibitors with IC50 of 115.2 μg mL−1, 182.2 μg mL−1 and 45.5 μg mL−1, respectively. In the PqsR system, no activity observed suggesting that the selectivity of the compound toward the LasB system. In addition, 7 showed the moderate anti-biofilm formation of Pseudomonas aeruginosa. Docking studies revealed that 3, 6 and 7 binding to the active site of Pseudomonas aeruginosa quorum sensing LasR system with better affinity compared to reference compounds 4-NPO. Finally, computation calculations suggest that compounds are a good template for further drug development. 2021-09-14T07:14:55Z 2021-09-14T07:14:55Z 2021 Bài trích https://pubs.rsc.org/en/content/articlelanding/2021/RA/D1RA03616E https://dlib.phenikaa-uni.edu.vn/handle/PNK/2865 https://doi.org/10.1039/D1RA03616E eng RSC advances
institution Digital Phenikaa
collection Digital Phenikaa
language eng
description Quorum sensing is a well-known term for describing bacterial cell–cell communication. Bacteria use quorum sensing pathways to respond to external factors such as nutrient availability, defense mechanisms, and coordinate host toxic behaviors such as biofilm formation, virulence production, and other pathogenesis. Discovery of novel compounds which inhibit quorum sensing without being antibiotic are currently emerging fields. Herein, the library of fifteen benzo[d]thiazole/quinoline-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl compounds was designed, synthesized and evaluated to find novel quorum sensing inhibitors. Firstly, compounds were evaluated for their growth inhibitory activities at high concentrations up to 1000 μg mL−1 toward Pseudomonas aeruginosa. Under our conditions, twelve compounds showed moderate growth inhibitory activities in the concentration tested. To our delight, three compounds 3, 6 and 7 do not affect the growth of the bacteria which were chosen for the evaluation of quorum sensing inhibitor activities. In the LasB system, our compounds 3, 6, 7 showed promising quorum-sensing inhibitors with IC50 of 115.2 μg mL−1, 182.2 μg mL−1 and 45.5 μg mL−1, respectively. In the PqsR system, no activity observed suggesting that the selectivity of the compound toward the LasB system. In addition, 7 showed the moderate anti-biofilm formation of Pseudomonas aeruginosa. Docking studies revealed that 3, 6 and 7 binding to the active site of Pseudomonas aeruginosa quorum sensing LasR system with better affinity compared to reference compounds 4-NPO. Finally, computation calculations suggest that compounds are a good template for further drug development.
format Bài trích
author Tung Truong Thanh
Huy Luong Xuan
Thang Nguyen Quoc
spellingShingle Tung Truong Thanh
Huy Luong Xuan
Thang Nguyen Quoc
Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria
author_facet Tung Truong Thanh
Huy Luong Xuan
Thang Nguyen Quoc
author_sort Tung Truong Thanh
title Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria
title_short Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria
title_full Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria
title_fullStr Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria
title_full_unstemmed Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria
title_sort benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasb quorum sensing inhibitors of gram-negative bacteria
publisher RSC advances
publishDate 2021
url https://pubs.rsc.org/en/content/articlelanding/2021/RA/D1RA03616E
https://dlib.phenikaa-uni.edu.vn/handle/PNK/2865
https://doi.org/10.1039/D1RA03616E
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score 8.891145

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