Integration of naturally bioactive thiazolium and 1,3,4-oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogates

Plant microbial diseases caused global production constraints have become one of the most challenging events, thus urgently needing to be addressed nowadays. To efficiently promote the discovery of promising antimicrobial surrogates, a type of 1,3,4-oxadiazole thioethers owning naturally bioactive t...

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Main Authors: Huai-He Zhu, Dan Zeng, Ming-Wei Wang, Pei-Yi Wang, Yuan-Yuan Wu, Li-Wei Liu, Song Yang
Format: Article
Language:English
Published: Springer 2020-01-01
Series:Journal of Saudi Chemical Society
Online Access:http://www.sciencedirect.com/science/article/pii/S1319610319301127
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author Huai-He Zhu
Dan Zeng
Ming-Wei Wang
Pei-Yi Wang
Yuan-Yuan Wu
Li-Wei Liu
Song Yang
author_facet Huai-He Zhu
Dan Zeng
Ming-Wei Wang
Pei-Yi Wang
Yuan-Yuan Wu
Li-Wei Liu
Song Yang
author_sort Huai-He Zhu
collection DOAJ
description Plant microbial diseases caused global production constraints have become one of the most challenging events, thus urgently needing to be addressed nowadays. To efficiently promote the discovery of promising antimicrobial surrogates, a type of 1,3,4-oxadiazole thioethers owning naturally bioactive thiazolium patterns was designed and fabricated. Antibacterial screening results revealed that title compounds could significantly inhibit the growth of pathogens Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, and Xanthomonas axonopodis pv. citri. And the related antibacterial efficacy was elevated by approximately 386-, 16-, and 24-folds comparing those of mainly used commercial agents bismerthiazol and thiodiazole copper. In vivo experiment suggested that A9 could manage rice bacterial blight with the corresponding curative and protection efficiencies of 48.01% and 50.55% at 200 μg/mL. Moreover, SEM patterns and fluorescence spectra were performed to explore the possible antibacterial mechanism. Preliminary antifungal bioassays revealed that these molecules paraded broad-spectrum inhibition effects against three tested fungal strains. Considering the simple molecular skeleton and significant biological actions, title compounds can be further explored as potential antimicrobial surrogates for managing plant bacterial and fungal diseases. Keywords: Thiazolium, 1,3,4-Oxadiazole, In vitro and in vivo bioassays, Antimicrobial
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institution Kabale University
issn 1319-6103
language English
publishDate 2020-01-01
publisher Springer
record_format Article
series Journal of Saudi Chemical Society
spelling doaj-art-baba89ba3ff2477184dc2c709672e4512025-08-20T03:49:04ZengSpringerJournal of Saudi Chemical Society1319-61032020-01-0124112713810.1016/j.jscs.2019.10.002Integration of naturally bioactive thiazolium and 1,3,4-oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogatesHuai-He Zhu0Dan Zeng1Ming-Wei Wang2Pei-Yi Wang3Yuan-Yuan Wu4Li-Wei Liu5Song Yang6State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, ChinaState Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, ChinaState Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, ChinaCorresponding authors.; State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, ChinaState Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, ChinaState Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, ChinaCorresponding authors.; State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, ChinaPlant microbial diseases caused global production constraints have become one of the most challenging events, thus urgently needing to be addressed nowadays. To efficiently promote the discovery of promising antimicrobial surrogates, a type of 1,3,4-oxadiazole thioethers owning naturally bioactive thiazolium patterns was designed and fabricated. Antibacterial screening results revealed that title compounds could significantly inhibit the growth of pathogens Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, and Xanthomonas axonopodis pv. citri. And the related antibacterial efficacy was elevated by approximately 386-, 16-, and 24-folds comparing those of mainly used commercial agents bismerthiazol and thiodiazole copper. In vivo experiment suggested that A9 could manage rice bacterial blight with the corresponding curative and protection efficiencies of 48.01% and 50.55% at 200 μg/mL. Moreover, SEM patterns and fluorescence spectra were performed to explore the possible antibacterial mechanism. Preliminary antifungal bioassays revealed that these molecules paraded broad-spectrum inhibition effects against three tested fungal strains. Considering the simple molecular skeleton and significant biological actions, title compounds can be further explored as potential antimicrobial surrogates for managing plant bacterial and fungal diseases. Keywords: Thiazolium, 1,3,4-Oxadiazole, In vitro and in vivo bioassays, Antimicrobialhttp://www.sciencedirect.com/science/article/pii/S1319610319301127
spellingShingle Huai-He Zhu
Dan Zeng
Ming-Wei Wang
Pei-Yi Wang
Yuan-Yuan Wu
Li-Wei Liu
Song Yang
Integration of naturally bioactive thiazolium and 1,3,4-oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogates
Journal of Saudi Chemical Society
title Integration of naturally bioactive thiazolium and 1,3,4-oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogates
title_full Integration of naturally bioactive thiazolium and 1,3,4-oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogates
title_fullStr Integration of naturally bioactive thiazolium and 1,3,4-oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogates
title_full_unstemmed Integration of naturally bioactive thiazolium and 1,3,4-oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogates
title_short Integration of naturally bioactive thiazolium and 1,3,4-oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogates
title_sort integration of naturally bioactive thiazolium and 1 3 4 oxadiazole fragments in a single molecular architecture as prospective antimicrobial surrogates
url http://www.sciencedirect.com/science/article/pii/S1319610319301127
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