期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 3, 页码 344-350出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.12.040
关键词
Triazoles; Antifungal activity; Drug-drug interactions; Tetrazole; CYP3A4
资金
- National Natural Science Foundation of China [21402223]
In this letter, we report our efforts to design, synthesize and evaluate biological activities of a series of novel hybridized compounds containing 1-tetrazole and 4-pyridinyl-1,2,4-triazole-3-one. An analysis of structure-activity data indicates that the target compounds with bulky and hydrophobic side chains exhibited stronger activities against the Candida spp and Cryptococcus neoformans tested than those of fluconazole and racemic VT-1161. Furthermore, 13k and 13ad were active against Microsporum gypseum, which was resistant to racemic VT-1161. In addition, 13k, 13ac and 13ad, with good in vitro activities against all of pathogenic fungi tested except for Aspergillus fumigatus, had no inhibition of human CYP3A4, suggesting a low risk of drug-drug interactions. (C) 2017 Elsevier Ltd. All rights reserved.
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