| Autor: |
Tingjunhong Ni, Lei Pang, Zhan Cai, Fei Xie, Zichao Ding, Yumeng Hao, Ran Li, Shichong Yu, Xiaoyun Chai, Ting Wang, Yongsheng Jin, Dazhi Zhang, Yuanying Jiang |
| Jazyk: |
angličtina |
| Rok vydání: |
2019 |
| Předmět: |
|
| Zdroj: |
Journal of Saudi Chemical Society, Vol 23, Iss 5, Pp 576-585 (2019) |
| Druh dokumentu: |
article |
| ISSN: |
1319-6103 |
| DOI: |
10.1016/j.jscs.2018.10.003 |
| Popis: |
In order to explore novel antifungal agents, twenty-seven triazole derivatives featuring an alkyne linker in the side chain were designed and synthesized by the Sonogashira reaction. Most of the target compounds exhibited good antifungal activity against eight human pathogenic fungi, especially excellent activity against Candida and Cryptococcus species, comparing with the reference drugs fluconazole, voriconazole and ravuconazole. Compounds A2 and A3 exhibited in vitro activity against all the tested fungi with MIC80 values ranging from 0.0156 μg/mL to 0.5 μg/mL, which are superior to ravuconazole and fluconazole. SAR and molecular docking study give a clear conclusion that para-fluoro, para-chloro, and para-cyano substituted phenylalkynyl or pyridinylalkynyl side chains may promote triazole antifungal activity. Keywords: Triazole, Alkyne, CYP51, Antifungal, Synthesis |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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