Synthesis and anti-Candida albicans activity of oleanolic acid derivatives.

IF 1.6 3区 医学 Q3 CHEMISTRY, APPLIED
Fei Zou, Lu-Yi Jiang, Fei Chen, Ze-Fei Fan, Tian-Yu Zhang, Tian-Yue Yang, Rui-Rui Wang, Guang-Hui Ni
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引用次数: 0

Abstract

With the increase incidence of Candida albicans infections and the widespread use of azole drugs, particularly fluconazole, the emergence of drug-resistant strains has become a significant concern. In this study, the derivatives were prepared by nucleophilic substitution at the 3-OH position of oleanolic acid, utilizing the reactivity of triphosgene, and by electrophilic coupling at the 28-COOH position through photoredox reactions. The antifungal activity of all compounds was evaluated, revealing that most derivatives exhibited good synergistic antifungal activity with fluconazole against the drug-resistant Candida albicans strain ATCC14053, with FICI values ranging from 0.45 to 0.14.

齐墩果酸衍生物的合成及抗白色念珠菌活性研究。
随着白色念珠菌感染发病率的增加和唑类药物特别是氟康唑的广泛使用,耐药菌株的出现已成为一个重大问题。本研究利用三光气的反应活性,在齐墩果酸的3-OH位置进行亲核取代,在28-COOH位置通过光氧化还原反应进行亲电偶联,制备了衍生物。对所有化合物的抗真菌活性进行了评价,结果表明大多数衍生物与氟康唑对耐药白色念珠菌菌株ATCC14053具有良好的协同抗真菌活性,其FICI值在0.45 ~ 0.14之间。
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来源期刊
CiteScore
3.20
自引率
5.90%
发文量
47
审稿时长
2.3 months
期刊介绍: The Journal of Asian Natural Products Research (JANPR) publishes chemical and pharmaceutical studies in the English language in the field of natural product research on Asian ethnic medicine. The journal publishes work from scientists in Asian countries, e.g. China, Japan, Korea and India, including contributions from other countries concerning natural products of Asia. The journal is chemistry-orientated. Major fields covered are: isolation and structural elucidation of natural constituents (including those for non-medical uses), synthesis and transformation (including biosynthesis and biotransformation) of natural products, pharmacognosy, and allied topics. Biological evaluation of crude extracts are acceptable only as supporting data for pure isolates with well-characterized structures. All published research articles in this journal have undergone rigorous peer review, based on initial editor screening and anonymized refereeing by at least two expert referees.
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