N-((2-苯氧恶唑-4-基)甲基)嘧啶类羧胺衍生物的设计、合成及生物学评价

IF 1.3 3区化学 Q3 CHEMISTRY, ORGANIC

Heterocyclic Communications Pub Date : 2020-01-01 DOI:10.1515/HC-2020-0117

Danling Huang, Shumin Zheng, Yong‐Xian Cheng

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引用次数: 4

摘要

设计、合成了12个N-((2-苯基氯唑-4-酰基)甲基)嘧啶类carboxamide衍生物，并通过1H NMR、13C NMR和HRMS对其进行了表征。对这些新化合物对菌核菌、灰孢菌和fragariae的抑菌活性进行了评价。结果表明，化合物5b、5f和5g对真菌有一定的杀灭活性，其中5f对菌核病菌的IC50值为28.9 mg/L。其中，化合物5f和5g的IC50值分别为54.8 mg/L和62.2 mg/L，表明其活性高于市售杀菌剂噻虫唑。讨论了表面的构效关系，对杀菌剂的开发和新型杀菌剂的发现有一定的指导意义。

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Design, Synthesis and Biological Evaluation of N-((2-phenyloxazol-4-yl)methyl) Pyrimidine Carboxamide Derivatives as Potential Fungicidal Agents

Twelve N-((2-phenyloxazol-4-yl)methyl) pyrimidine carboxamide derivatives were designed, synthesized, and characterized by 1H NMR, 13C NMR, and HRMS. The fungicidal activities of these new compounds against Sclerotinia sclerotiorum, Botrytis cinereal, and Colletotrichum fragariae were evaluated. The results indicated that compounds 5b, 5f, and 5g displayed potential fungicidal activities against tested fungi, especially 5f exhibited IC50 value of 28.9 mg/L against S. sclerotiorum. Moreover, the compounds 5f and 5g showed IC50 values of 54.8 mg/L and 62.2 mg/L against C. fragariae respectively, which shows that they were more active than the commercial fungicide hymexazol. The superficial structure-activity relationships were discussed, which may be of benefit for the development of fungicides and discovery of novel fungicides.

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来源期刊

Heterocyclic Communications 化学-有机化学

CiteScore

3.80

自引率

4.30%

发文量

审稿时长

1.4 months

期刊介绍： Heterocyclic Communications (HC) is a bimonthly, peer-reviewed journal publishing preliminary communications, research articles, and reviews on significant developments in all phases of heterocyclic chemistry, including general synthesis, natural products, computational analysis, considerable biological activity and inorganic ring systems. Clear presentation of experimental and computational data is strongly emphasized. Heterocyclic chemistry is a rapidly growing field. By some estimates original research papers in heterocyclic chemistry have increased to more than 60% of the current organic chemistry literature published. This explosive growth is even greater when considering heterocyclic research published in materials science, physical, biophysical, analytical, bioorganic, pharmaceutical, medicinal and natural products journals. There is a need, therefore, for a journal dedicated explicitly to heterocyclic chemistry and the properties of heterocyclic compounds.