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首页> 外文期刊>Archiv der Pharmazie >Synthesis, antimicrobial evaluation, and docking studies of novel 4-substituted quinazoline derivatives as DNA-gyrase inhibitors.
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Synthesis, antimicrobial evaluation, and docking studies of novel 4-substituted quinazoline derivatives as DNA-gyrase inhibitors.

机译：合成，抗菌评估和对接研究作为DNA回转酶抑制剂的新型4-取代的喹唑啉衍生物。

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摘要

Quinazoline derivatives are reported to have anti-inflammatory, analgesic, antibacterial, and anticancer activities. The incorporation of "OCHCONH" (oxymethylcarbamide) at 4th position of the quinazoline ring was found to influence the biological activities of the molecules. With this rationale, some new oxadiazolyl methyloxy quinazolines, pyrazolyl acetoxy methyl quinazolines, triazolylmethyloxy quinazolines were synthesized from anthranilic acid through quinazolyl oxyacetylhydrazide intermediates. All the compounds were characterized by IR, (1)H-NMR, EI-MS, and C, H, N analyses and evaluated for their antimicrobial activity. Docking studies on the DNA-gyrase enzyme (1KZN) show their role in the antimicrobial activity of the molecules and explain the higher potency of compounds 6a, 6b, 8a, 8b based on ReRanking scores and binding poses of the molecules.
机译：据报道，喹唑啉衍生物具有抗炎，止痛，抗菌和抗癌活性。发现在喹唑啉环的第4位上掺入“ OCHCONH”（氧甲基脲）会影响分子的生物学活性。根据这一原理，由邻氨基苯甲酸通过喹唑基氧基乙酰肼中间体制备了一些新的恶二唑基甲氧基喹唑啉，吡唑基乙酰氧基甲基喹唑啉，三唑基甲氧基喹唑啉。所有化合物均通过IR，（1）H-NMR，EI-MS和C，H，N分析进行表征，并评估其抗菌活性。对DNA旋回酶（1KZN）的对接研究显示了它们在分子的抗菌活性中的作用，并基于分子的ReRanking得分和结合姿势解释了化合物6a，6b，8a，8b的更高效力。

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