LI Yang-yang, LIU Hua, LIU Hong, ZHANG Yong-qiang, ZHANG Wan-nian, SHENG Chun-quan. Design, synthesis and antifungal activity of novel triazole derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(1): 27-31. doi: 10.3969/j.issn.1006-0111.2013.01.008
| Citation:
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LI Yang-yang, LIU Hua, LIU Hong, ZHANG Yong-qiang, ZHANG Wan-nian, SHENG Chun-quan. Design, synthesis and antifungal activity of novel triazole derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(1): 27-31. doi: 10.3969/j.issn.1006-0111.2013.01.008
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Design, synthesis and antifungal activity of novel triazole derivatives
- 1.
Department of Medicinal Chemistry, Jiangxi institute of traditional Chinese medicine, Nanchang 330006, China
- 2.
Department of Medicinal Chemistry, Second Military Medicinal University, Shanghai 200433, China
- Received Date: 2012-06-01
- Rev Recd Date:
2012-09-21
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Abstract
Objective To design the novel triazole derivatives and test their in vitro antifungal activities on the basis of the molecular design model for rational optimization of azole drugs. Methods Ring-open reaction of the oxiranes was used to synthesize the target compounds, whose chemical structures were confirmed by 1H NMR and MS. Serial dilution method was used to determine the in vitro antifungal activities. Results Two novel azole compounds containing trizaolone side chains were synthesized which showed excellent and broad-spectrum antifungal activity. Conclusion The targeted compounds showed better antifungal activity against Candida albicans than the positive drugs fluconazole and ketoconazole, which was worth to further investigate the structure-activity relationship.
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