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喹唑啉-4(3)-酮功能化共轭银纳米颗粒的抗菌作用

Antibacterial Effects of Quinazolin-4(3)-One Functionalized-Conjugated Silver Nanoparticles.

作者信息

Masri Abdulkader, Anwar Ayaz, Khan Naveed Ahmed, Shahbaz Muhammad Saquib, Khan Khalid Mohammed, Shahabuddin Syed, Siddiqui Ruqaiyyah

机构信息

Department of Biological Sciences, School of Science and Technology, Sunway University, Selangor 47500, Malaysia.

HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi City, Sindh 75270, Pakistan.

出版信息

Antibiotics (Basel). 2019 Oct 9;8(4):179. doi: 10.3390/antibiotics8040179.

Abstract

Infections due to multi-drug resistant bacteria are on the rise and there is an urgent need to develop new antibacterials. In this regard, a series of six functionally diverse new quinazolinone compounds were synthesized by a facile one-pot reaction of benzoic acid derivatives, trimethoxymethane and aniline derivatives. Three compounds of 3-aryl-8-methylquinazolin-4(3H)-one, and 3-aryl-6,7-dimethoxyquinazolin4(3H)-one were prepared and tested against multi-drug resistant bacteria. Furthermore, we determined whether conjugation with silver nanoparticles improved the antibacterial efficacy of these quinazolinone derivatives. The newly synthesized compounds were characterized by ultraviolet visible spectrophotometry (UV-vis), Zetasizer analysis, Fourier transform infrared spectroscopic methods (FT-IR), and scanning electron microscopy (SEM). Using bactericidal evaluation, effects were determined against selected Gram-negative and Gram-positive bacteria. Furthermore, cytotoxicity of nanoconjugates on human cells were determined. The UV-vis spectrum of silver nanoparticles conjugated quinazolinone displayed surface plasmon resonance band in the range of 400-470 nm, and the size of nanoparticles was detected to be in the range of 100-250 nm by dynamic light scattering (DLS). FT-IR study confirmed the stabilization of silver nanoparticles by the presence of diverse functional arayl on each compound. SEM further revealed the construction of spherical nanoparticles. Among the quinazolinone derivative tested, two compounds (QNZ 4, QNZ 6) conjugated with silver nanoparticles showed enhanced antibacterial activity against K1, , , and as compared to the compounds.

摘要

耐多药细菌引起的感染正在增加,迫切需要开发新的抗菌药物。在这方面,通过苯甲酸衍生物、三甲氧基甲烷和苯胺衍生物的简便一锅反应合成了一系列六种功能多样的新型喹唑啉酮化合物。制备了三种3-芳基-8-甲基喹唑啉-4(3H)-酮和3-芳基-6,7-二甲氧基喹唑啉-4(3H)-酮化合物,并对耐多药细菌进行了测试。此外,我们还确定了与银纳米颗粒结合是否能提高这些喹唑啉酮衍生物的抗菌效果。通过紫外可见分光光度法(UV-vis)、Zetasizer分析、傅里叶变换红外光谱法(FT-IR)和扫描电子显微镜(SEM)对新合成的化合物进行了表征。通过杀菌评估,确定了对选定的革兰氏阴性菌和革兰氏阳性菌的作用。此外,还测定了纳米缀合物对人细胞的细胞毒性。银纳米颗粒共轭喹唑啉酮的UV-vis光谱在400-470nm范围内显示表面等离子体共振带,通过动态光散射(DLS)检测到纳米颗粒的尺寸在100-250nm范围内。FT-IR研究证实了每种化合物上不同官能团芳基的存在使银纳米颗粒得以稳定。SEM进一步揭示了球形纳米颗粒的结构。在所测试的喹唑啉酮衍生物中,与银纳米颗粒结合的两种化合物(QNZ 4、QNZ 6)对K1、、、和的抗菌活性比未结合的化合物增强。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d50c/6963639/4017a0ac6547/antibiotics-08-00179-g001.jpg

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