Discovery of Quinazoline-2,4(1H,3H)-Dione Derivatives as Potential Antibacterial Agent: Design, Synthesis, and Their Antibacterial Activity

被引:9
作者
Boshta, Nader M. [1 ]
El-Essawy, Farag A. [2 ]
Alshammari, Mohammed B. [3 ]
Noreldein, Safaa G. [1 ]
Darwesh, Osama M. [4 ]
机构
[1] Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32511, Egypt
[2] Prince Sattam Bin Abdulaziz Univ, Dept Basic Sci, Preparatory Year Deanship, POB 151, Alkharj 11942, Saudi Arabia
[3] Prince Sattam Bin Abdulaziz Univ, Coll Sci & Humanities, POB 151, Alkharj 11942, Saudi Arabia
[4] Natl Res Ctr, Agr Microbiol Dept, Environm Microbiol & Nanotechnol Grp, Cairo 12622, Egypt
关键词
synthesis; quinazoline; quinazoline-2; 4(1H; 3H)-dione; antimicrobial; fluoroquinolones; RESISTANT STAPHYLOCOCCUS-AUREUS; TOPOISOMERASE-IV; IN-VITRO; QUINAZOLINEDIONE SULFONAMIDES; ANTIMICROBIAL ACTIVITY; DNA GYRASE; INHIBITORS; BINDING; ANTAGONIST; QUINOLONES;
D O I
10.3390/molecules27123853
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
In this paper, we report on the design and synthesis of a novel series of quinazoline-2,4(1H,3H)-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(1H,3H)-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 13 and 15 provided broad bioactive spectrum against Gram-positive and Gram-negative strains compared to the standard drugs.
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页数:15
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