作者
KMA El-Gamal, FF Sherbiny, AM El-Morsi, HE Abu-El-khair, IH Eissa, MM El-Sebaei
发表日期
2015
期刊
Pharm Pharmacol Int J
卷号
2
期号
5
页码范围
165-177
简介
In an attempt to find new bio-active antimicrobial molecules, a series of quinoline-3-carbonitrile and 2-chloroquinoline derivatives were synthesized by multistep reactions. The new compounds were characterized by IR, 1H NMR and mass spectra. Antimicrobial screening of title compounds (3-24) was carried out against Grampositive and Gram negative bacteria and fungi using agar diffusion technique. To understand the interaction of binding sites with bacterial protein receptor, the docking study was performed using topoisomerase II DNA gyrase enzymes. The newly synthesized compounds 14, 10 and 22 showed significant potency against different bcterial strains compared with Ciprofloxacine, Ampicillin and Gentamicin. While compounds 14, 22 and 6d had strong antifungal activity comparable to Amphotericin B. The results of in vitro antimicrobial activity and docking study revealed that the synthesized compounds have potential antimicrobial activity and can be further optimized and developed as a lead compound.
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