Design and synthesis of novel antifungal triazole derivatives with good activity and water solubility |
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Authors: | Xu-Feng Cao Wen-Jing Chu Yong-Bing Cao Yu-She Yang |
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Institution: | a State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 20103, China;
b School of Pharmacy, Second Military Medical University, Shanghai 200433, China |
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Abstract: | In order to find novel antifungal agents with good activity and aqueous solubility, a series of SYN-2869 analogues containing a pyridine ring were synthesized and evaluated for their in vitro antifungal activity and water solubility. The results indicated that some compounds showed potent activity against six pathogenic fungi. In particular, the analogue 17a having an isobutyl substitution on the triazolone exhibited significant broad spectrum antifungal activity. In addition, the water solubility of compound 17a was sufficiently improved over SYN-2869. |
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Keywords: | Synthesis Antifungal SYN-2869 analogues Triazole Water solubility |
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