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首页> 外文期刊>Archiv der Pharmazie >Design and synthesis of novel benzopyran-2-one derivatives of expected antimicrobial activity through DNA gyrase-B inhibition.
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Design and synthesis of novel benzopyran-2-one derivatives of expected antimicrobial activity through DNA gyrase-B inhibition.

机译：设计和合成新的苯并吡喃-2-酮衍生物，具有预期的抗菌活性，可通过DNA旋转酶B抑制。

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摘要

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 (beta-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.
机译：为了找到一类新的抗菌剂，我们合成了三十种新的香豆素（2H-苯并吡喃-2-酮）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通过氧乙酰氨基或氧甲基桥连接成4-苯基-2H-苯并吡喃-2-酮。从2-氧代-4-苯基-2H-苯并[b]吡喃-7-基-氧乙酸酰肼2a-f开始合成目标化合物。通过分子建模和对接技术，使用Molsoft ICM 3.4-8C程序将新化合物评估为DNA促旋酶B抑制剂。还筛选了合成的化合物对四种不同革兰氏阳性菌和革兰氏阴性菌的抗菌活性。以及针对白色念珠菌的抗真菌活性进行筛选。分子模型数据与抗菌筛选结果一致。

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