Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Koam 32511, Egypt.
Preparatory Year Deanship, Basic Science Department, Prince Sattam Bin Abdulaziz University, P.O. Box 151, Alkharj 11942, Saudi Arabia.
Molecules. 2022 Jun 15;27(12):3853. doi: 10.3390/molecules27123853.
In this paper, we report on the design and synthesis of a novel series of quinazoline-2,4(1,3)-dione derivatives as fluoroquinolone-like inhibitors of bacterial gyrase and DNA topoisomerase IV to identify and develop antimicrobial agents to prevent bacterial resistance problems. Their structures were confirmed using spectroscopic analyses (IR, NMR, and EI-MS). The novel quinazoline-2,4(1,3)-dione derivatives were evaluated for their antimicrobial activities against Gram-positive and Gram-negative bacterial strains using the Agar well diffusion method to study the antimicrobial activities and compared them with the standard drugs. Most compounds displayed moderate activity. Among the tested compounds, the most promising compounds and provided broad bioactive spectrum against Gram-positive and Gram-negative strains compared to the standard drugs.
本文报告了一系列新型喹唑啉-2,4(1,3)-二酮衍生物的设计和合成,它们是氟喹诺酮类细菌拓扑异构酶 II 和 IV 的抑制剂,旨在发现和开发抗菌药物以预防细菌耐药性问题。它们的结构通过光谱分析(IR、NMR 和 EI-MS)得到确认。采用琼脂孔扩散法评价了新型喹唑啉-2,4(1,3)-二酮衍生物对革兰氏阳性和革兰氏阴性细菌菌株的抗菌活性,以研究抗菌活性,并与标准药物进行比较。大多数化合物表现出中等活性。在所测试的化合物中,与标准药物相比,最有前途的化合物 和 对革兰氏阳性和革兰氏阴性菌株具有广泛的生物活性谱。