Design, synthesis, and anti-oomycete activity of 3-acyloxymaltol/ethyl maltol derivatives

IF 1.3 3区医学 Q3 CHEMISTRY, APPLIED

Journal of Asian Natural Products Research Pub Date : 2024-06-10 DOI:10.1080/10286020.2024.2355144

引用次数: 0

Abstract

Twenty 3-acyloxymaltol/ethyl maltol derivatives (7a-j and 8a-j) were synthesized and evaluated in vitro for their anti-oomycete activity against Phytophthora capsici, respectively. Among all of twenty derivatives, more than half of the compounds 7f, 7h, 8a-h and 8j had anti-oomycete activity higher than the positive control zoxamide (EC₅₀ = 22.23 mg/L), and the EC₅₀ values of 18.66, 20.32, 12.80, 16.18, 10.59, 14.98, 16.80, 10.36, 15.32, 12.64, and 13.59 mg/L, respectively. Especially, compounds 8c and 8f exhibited the best anti-oomycete activity against P. capsici with EC₅₀ values of 10.59 and 10.36 mg/L, respectively. Overall, hydroxyl group of maltol/ethyl maltol is important active modification site.

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3-acyloxymaltol/ethyl maltol 衍生物的设计、合成和抗霉菌活性。

合成了 20 种 3-乙酰氧基麦芽酚/乙基麦芽酚衍生物（7a-j 和 8a-j），并分别在体外评估了它们对蝙蝠蛾属真菌的抗真菌活性。在所有 20 个衍生物中，超过半数的化合物 7f、7h、8a-h 和 8j 的抗真菌活性高于阳性对照佐酰胺（EC50 = 22.23 mg/L），EC50 值分别为 18.66、20.32、12.80、16.18、10.59、14.98、16.80、10.36、15.32、12.64 和 13.59 mg/L。特别是化合物 8c 和 8f 对荚膜蘑菇菌的抗真菌活性最好，EC50 值分别为 10.59 和 10.36 毫克/升。总之，麦芽酚/乙基麦芽酚的羟基是重要的活性修饰位点。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Asian Natural Products Research 医学-药学

CiteScore

3.20

自引率

5.90%

发文量

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.