Abstract A series of pyrimidine‐containing 4 H ‐chromen‐4‐one derivatives were designed and synthesized by combining bioactive substructures. Preliminary biological activity results showed that most of the compounds displayed significant inhibitory activities in vitro against Xanthomonas axonopodis pv. Citri ( X. axonopodis ), Xanthomonas oryzae pv. oryzae ( X. oryzae ) and Ralstonia solanacearum ( R. solanacearum ). In particular, compound 2‐[(3‐{[5,7‐dimethoxy‐4‐oxo‐2‐(3,4,5‐trimethoxyphenyl)‐4 H ‐1‐benzopyran‐3‐yl]oxy}propyl)sulfanyl]‐4‐(4‐methylphenyl)‐6‐oxo‐1,6‐dihydropyrimidine‐5‐carbonitrile ( 4c ) demonstrated a good inhibitory effect against X. axonopodis and X. oryzae , with the half‐maximal effective concentration (EC 50 ) values of 15.5 and 14.9 μg/mL, respectively, and compound 2‐[(3‐{[5,7‐Dimethoxy‐4‐oxo‐2‐(3,4,5‐trimethoxyphenyl)‐4 H ‐1‐benzopyran‐3‐yl]oxy}propyl)sulfanyl]‐4‐(3‐fluorophenyl)‐6‐oxo‐1,6‐dihydropyrimidine‐5‐carbonitrile ( 4h ) showed the best antibacterial activity against R. solanacearum with an EC 50 value of 14.7 μg/mL. These results were better than commercial reagents bismerthiazol (BT, 51.7, 70.1 and 52.7 μg/mL, respectively) and thiodiazole copper (TC, 77.9, 95.8 and 72.1 μg/mL, respectively). In vivo antibacterial activity results indicated that compound 4c displayed better curative (42.4 %) and protective (49.2 %) activities for rice bacterial leaf blight than BT (35.2, 39.1 %) and TC (30.8, 27.3 %). The mechanism of compound 4c against X. oryzae was analyzed through scanning electron microscopy (SEM). These results indicated that pyrimidine‐containing 4 H ‐chromen‐4‐one derivatives have important value in the research of new agrochemicals.

Shijun Su

Mei Chen

Xuemei Tang

Feng Peng

Tingting Liu

Qing Zhou

Wenliang Zhan

Ming He

Chengwei Xie

Wei Xue

Chemistry & Biodiversity

化学与生物多样性是一个高质量的出版论坛，涵盖了广泛的生物相关主题，面向真正的国际受众。该杂志以完整的原创论文、简短的交流、特邀评论和评论的形式发表关于生物相关化学研究各个方面的特定领域和跨学科贡献。它涵盖了跨越化学和生物科学边界的所有研究领域，最终目标是拓宽我们对自然如何在分子水平上运作的理解。自 2017 年以来，《化学与生物多样性》以仅在线形式出版。

Chemistry and Biodiversity is a high-quality publication forum that covers a wide range of biology-related topics aimed at a truly international audience. The journal publishes original research articles, brief communications, invited reviews, and commentaries on various aspects of chemistry related to biological research, contributing to specific fields and interdisciplinary studies. It encompasses all research areas that cross the boundaries of chemistry and biological sciences, with the ultimate goal of broadening our understanding of how nature operates at the molecular level. Since 2017, Chemistry and Biodiversity has been published exclusively online.

《化学与生物多样性》是一个高质量的出版论坛，涵盖广泛的生物相关主题，面向国际受众。该杂志以完整的原创论文、简短的交流、特邀评论和综述的形式，发表关于生物相关化学研究各个方面的特定领域和跨学科的贡献。它涵盖了跨越化学和生物科学边界的所有研究领域，最终目标是拓宽我们对自然在分子水平上运作的理解。自2017年以来，《化学与生物多样性》仅以在线形式出版。

Chemistry and Biodiversity

Chemistry &amp; Biodiversity

Design, Synthesis and Antibacterial Activity of Novel Pyrimidine‐Containing 4<i>H</i>‐Chromen‐4‐One Derivatives**

In vivo antibacterial activity results indicated that pyrimidine-containing 4H-chromen-4-one derivatives have important value in the research of new agrochemicals.

Category	Quartile
化学	3
化学, 化学综合	3
化学, 生化与分子生物学	4

Design, Synthesis and Antibacterial Activity of Novel Pyrimidine‐Containing 4H‐Chromen‐4‐One Derivatives**

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Journal Info

Category	Quartile
CHEMISTRY, MULTIDISCIPLINARY	3