In an attempt to find a new class of antibacterial agents, we have synthesized thirty new coumarin (2H‐benzopyran‐2‐one) analogues. These derivatives include substituted azetidin‐2‐ones (β‐lactam) 3a–f, pyrrolidin‐2‐ones 4a–f, 2H‐1,3,4‐oxadiazoles 5a–f, and thiazolidin‐4‐ones 6a–f attached to 4‐phenyl‐2H‐benzopyran‐2‐one through an oxyacetamido or an oxymethyl bridge. The target compounds were synthesized starting from 2‐oxo‐4‐phenyl‐2H‐benzo[b]pyran‐7‐yl‐oxyacetic acid hydrazides 2a–f. The new compounds were evaluated as DNA gyrase‐B inhibitors through molecular modeling and docking techniques using the Molsoft ICM 3.4‐8C program. The synthesized compounds were also screened for antibacterial activity against four different species of Gram‐positive and Gram‐negative bacteria; as well as screening against C. albicans for antifungal activity. The molecular modeling data were in accordance with the antimicrobial screening results.

中文翻译：

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通过 DNA 旋转酶 B 抑制设计和合成具有预期抗菌活性的新型 Benzopyran-2-one 衍生物

为了寻找一类新的抗菌剂，我们合成了 30 种新的香豆素（2H-苯并吡喃-2-one）类似物。这些衍生物包括取代的氮杂环丁烷-2-酮（β-内酰胺）3a-f、吡咯烷-2-酮 4a-f、2H-1,3,4-恶二唑 5a-f 和噻唑烷-4-酮 6a-f 4-苯基-2H-苯并吡喃-2-one 通过氧乙酰氨基或氧甲基桥。以2-氧代-4-苯基-2H-苯并[b]吡喃-7-基-氧乙酸酰肼2a-f为原料合成目标化合物。使用 Molsoft ICM 3.4-8C 程序，通过分子建模和对接技术将新化合物评估为 DNA 促旋酶-B 抑制剂。还筛选了合成的化合物对四种不同种类的革兰氏阳性菌和革兰氏阴性菌的抗菌活性；以及筛选白色念珠菌的抗真菌活性。