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Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains
A series of triazole derivatives containing phenylethynyl pyrazole moiety as side chain were designed, synthesized, and most of them exhibited good in vitro antifungal activities. Especially, compounds 5k and 6c showed excellent in vitro activities against C. albicans (MIC = 0.125, 0.0625 μg/mL), C....
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9182106/ https://www.ncbi.nlm.nih.gov/pubmed/35684308 http://dx.doi.org/10.3390/molecules27113370 |
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author | Ni, Tingjunhong Ding, Zichao Xie, Fei Hao, Yumeng Bao, Junhe Zhang, Jingxiang Yu, Shichong Jiang, Yuanying Zhang, Dazhi |
author_facet | Ni, Tingjunhong Ding, Zichao Xie, Fei Hao, Yumeng Bao, Junhe Zhang, Jingxiang Yu, Shichong Jiang, Yuanying Zhang, Dazhi |
author_sort | Ni, Tingjunhong |
collection | PubMed |
description | A series of triazole derivatives containing phenylethynyl pyrazole moiety as side chain were designed, synthesized, and most of them exhibited good in vitro antifungal activities. Especially, compounds 5k and 6c showed excellent in vitro activities against C. albicans (MIC = 0.125, 0.0625 μg/mL), C. neoformans (MIC = 0.125, 0.0625 μg/mL), and A. fumigatus (MIC = 8.0, 4.0 μg/mL). Compound 6c also exerted superior activity to compound 5k and fluconazole in inhibiting hyphae growth of C. albicans and inhibiting drug-resistant strains of C. albicans, and it could reduce fungal burdens in mice kidney at a dosage of 1.0 mg/kg. An in vivo efficacy evaluation indicated that 6c could effectively protect mice models from C. albicans infection at doses of 0.5, 1.0, and 2.0 mg/kg. These results suggested that compound 6c deserves further investigation. |
format | Online Article Text |
id | pubmed-9182106 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-91821062022-06-10 Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains Ni, Tingjunhong Ding, Zichao Xie, Fei Hao, Yumeng Bao, Junhe Zhang, Jingxiang Yu, Shichong Jiang, Yuanying Zhang, Dazhi Molecules Article A series of triazole derivatives containing phenylethynyl pyrazole moiety as side chain were designed, synthesized, and most of them exhibited good in vitro antifungal activities. Especially, compounds 5k and 6c showed excellent in vitro activities against C. albicans (MIC = 0.125, 0.0625 μg/mL), C. neoformans (MIC = 0.125, 0.0625 μg/mL), and A. fumigatus (MIC = 8.0, 4.0 μg/mL). Compound 6c also exerted superior activity to compound 5k and fluconazole in inhibiting hyphae growth of C. albicans and inhibiting drug-resistant strains of C. albicans, and it could reduce fungal burdens in mice kidney at a dosage of 1.0 mg/kg. An in vivo efficacy evaluation indicated that 6c could effectively protect mice models from C. albicans infection at doses of 0.5, 1.0, and 2.0 mg/kg. These results suggested that compound 6c deserves further investigation. MDPI 2022-05-24 /pmc/articles/PMC9182106/ /pubmed/35684308 http://dx.doi.org/10.3390/molecules27113370 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Ni, Tingjunhong Ding, Zichao Xie, Fei Hao, Yumeng Bao, Junhe Zhang, Jingxiang Yu, Shichong Jiang, Yuanying Zhang, Dazhi Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains |
title | Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains |
title_full | Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains |
title_fullStr | Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains |
title_full_unstemmed | Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains |
title_short | Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains |
title_sort | design, synthesis, and in vitro and in vivo antifungal activity of novel triazoles containing phenylethynyl pyrazole side chains |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9182106/ https://www.ncbi.nlm.nih.gov/pubmed/35684308 http://dx.doi.org/10.3390/molecules27113370 |
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