用于抗菌和抗念珠菌活性的新型唑官能化聚甲基丙烯酸缩水甘油酯的合成与表征

Synthesis and Characterization of Novel Azole Functionalized Poly(glycidyl methacrylate)s for Antibacterial and Anticandidal Activity.

作者信息

Rehman Suriya, Gunday Seyda T, Alsalem Zainab H, Bozkurt Ayhan

机构信息

Epidemic Disease Research Department, Institute for Research & Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia.

Department of Biophysics, Institute for Research & Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia.

出版信息

Curr Org Synth. 2019;16(7):1002-1009. doi: 10.2174/1385272823666190828112113.

DOI:10.2174/1385272823666190828112113

PMID:31984881

Abstract

BACKGROUND

Presently, rise in the infectious diseases and subsequent development of drug resistance, is a global threat to human health. However, much efforts are being made by scientists, to develop novel antimicrobials, and also to improve the efficacy of available drugs, in order to combat the lifethreatening infections.

OBJECTIVE

Synthesis and characterization of azole functional polymer systems for antimicrobial applications.

MATERIALS AND METHODS

Poly(glycidyl methacrylate) (PGMA), was produced by free radical polymerization of the monomer, glycidyl methacrylate (GMA). Different azole functional PGMAs were produced, through chemical modification with imidazole (Im), 1H-1,2,4-triazole (Tri) and 3-amino-1,2,4-triazole (ATri), to get PGMA-Imi, PGMA-Tri and PGMA-ATri, respectively. The structure was confirmed by Fourier transform infrared spectroscopy (FT-IR), thermal properties were investigated by Thermogravimetric Analysis (TGA), and surface morphology was studied by scanning electron microscopy (SEM). Newly synthesized derivatives were further explored, for their antibacterial and anticandidal activities.

RESULTS

All the three synthesized and characterized derivatives, displayed a significant activity against the tested microorganisms. The minimum inhibitory concentration (MIC) and minimum bactericidal/fungicidal concentration (MBC/MFC), recorded against Staphylococcus aureus (S. aureus), was 0.5 &1mg/ml for PGMA-Imi, followed by PGMA-ATri & PGMA-Tri, respectively, followed by E. coli with, 1 & 2 mg/ml, 4 & 8 mg/ml, 4& 8 mg/ml, respectively, whereas the maximum MIC & MFC was recorded against C. albicans i.e., 8 & 16 mg/ml, 4 & 8 mg/ml ,4 & 8 mg/ml for PGMA-ATri, PGMA-Tri, PGMA-Imi, respectively.

CONCLUSION

In the present work, we report on the state-of-the-art, azole functional polymer systems for antimicrobial applications. These findings suggest that the synthesized azole functional polymer films have antimicrobial properties, which could be potential candidates for coating applications in the biomedical and wastewater treatment field.

摘要

背景

目前，传染病的增加以及随后耐药性的产生，是对人类健康的全球威胁。然而，科学家们正在做出巨大努力，开发新型抗菌药物，并提高现有药物的疗效，以对抗危及生命的感染。

目的

合成并表征用于抗菌应用的唑功能聚合物体系。

材料与方法

通过甲基丙烯酸缩水甘油酯（GMA）单体的自由基聚合制备聚甲基丙烯酸缩水甘油酯（PGMA）。通过用咪唑（Im）、1H-1,2,4-三唑（Tri）和3-氨基-1,2,4-三唑（ATri）进行化学改性，分别得到不同的唑功能化PGMA，即PGMA-Imi、PGMA-Tri和PGMA-ATri。通过傅里叶变换红外光谱（FT-IR）确认结构，通过热重分析（TGA）研究热性能，通过扫描电子显微镜（SEM）研究表面形态。进一步探索新合成的衍生物的抗菌和抗念珠菌活性。

结果

所有三种合成并表征的衍生物对测试微生物均显示出显著活性。针对金黄色葡萄球菌（S. aureus）记录的最低抑菌浓度（MIC）和最低杀菌/杀真菌浓度（MBC/MFC），PGMA-Imi分别为0.5和1mg/ml，其次是PGMA-ATri和PGMA-Tri，针对大肠杆菌的分别为1和2mg/ml、4和8mg/ml、4和8mg/ml，而针对白色念珠菌记录的最大MIC和MFC，PGMA-ATri、PGMA-Tri、PGMA-Imi分别为8和16mg/ml、4和8mg/ml、4和8mg/ml。