合成的2-甲基硫代苯并[g][1,2,4]-三唑并[1,5-a]喹唑啉衍生物的抗菌活性
Antimicrobial Activity of Synthesized 2-Methylthiobenzo[g][1,2,4]- triazolo[1,5-a]quinazoline Derivatives.
作者信息
Al-Salahi Rashad, Abuelizz Hatem A, Wadi Mahasin, El Dib Rabab A, Alotaibi Mshari A, Marzouk Mohamed
机构信息
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. box 2457, Riyadh 11451, Saudi Arabia.
出版信息
Med Chem. 2016;12(8):760-766. doi: 10.2174/1573406412666160502155106.
BACKGROUND
The present study was carried out to evaluate the antimicrobial activity of a synthesized 2-methylthio-benzo[g][1,2,4]triazolo[1,5- a]quinazoline series. The compounds (1-21) were tested against a variety of Gram-positive bacterial species including Bacillus subtilis (RCMB 01001 69-3), Enterococcus faecalis (RCMB 0100154-2), Staphylococcus aureus (RCMB 0100183-9), Staphylococcus epidermidis (RCMB 0100183-9) and Streptococcus pyogenes (RCMB 0100172-5). In addition, Gram-negative bacteria were also tested including Pseudomonas aeruginosa (RCMB 0100243-5), Escherichia coli (RCMB 010052-6), Proteus mirabilis (RCMB 01002 54-2), Klebsiella oxytoca (RCMB 01002 83-4) and Enterobacter cloacae (RCMB 01002 64-5). Furthermore, their activities were screened against ten types of fungi i.e. Aspergillus fumigatus (RCMB 02568), Syncephalastrum racemosum (RCMB 05922), Geotricum candidum (RCMB 05097), Candida albicans (RCMB 05036), Aspergillus niger (RCMB 02724), Cryptococcus neoformans (RCMB 05642), Candida tropicalis (RCMBA 05239), Penicillium expansum (RCMB 01924), Microsporum canis (RCMB 0834) and Trichophyton mentagrophytes (RCMB 0925).
METHODS
Evaluation of antimicrobial activity was performed using agar well diffusion method in comparison with ampicillin and gentamycin as antibacterial reference drugs, and amphotericin B as antifungal reference drug. The minimum inhibitory concentration (MIC) was determined using the broth double dilution technique.
RESULTS
The MIC values of the tested compounds were reported in .g/mL in which ampicillin, gentamicin and amphotericin B were used as standard reference drugs. The obtained results revealed that compounds 3, 4, 7, 8, 9, 10, 11, 14, 17, 18, 19, 20 and 21 showed significant antimicrobial activity against six bacterial and six fungal strains.
CONCLUSION
The promising compounds could be employed as useful scaffolds for building of new derivatives with more potent antimicrobial effects.
背景
本研究旨在评估合成的2-甲硫基-苯并[g][1,2,4]三唑并[1,5-a]喹唑啉系列化合物的抗菌活性。对化合物（1-21）针对多种革兰氏阳性细菌进行了测试，包括枯草芽孢杆菌（RCMB 01001 69-3）、粪肠球菌（RCMB 0100154-2）、金黄色葡萄球菌（RCMB 0100183-9）、表皮葡萄球菌（RCMB 0100183-9）和化脓性链球菌（RCMB 0100172-5）。此外，还对革兰氏阴性细菌进行了测试，包括铜绿假单胞菌（RCMB 0100243-5）、大肠杆菌（RCMB 010052-6）、奇异变形杆菌（RCMB 01002 54-2）、产酸克雷伯菌（RCMB 01002 83-4）和阴沟肠杆菌（RCMB 01002 64-5）。此外，还针对十种真菌筛选了它们的活性，即烟曲霉（RCMB 02568）、总状共头霉（RCMB 05922）、白地霉（RCMB 05097）、白色念珠菌（RCMB 05036）、黑曲霉（RCMB 02724）、新型隐球菌（RCMB 05642）、热带念珠菌（RCMBA 05239）、扩展青霉（RCMB 01924）、犬小孢子菌（RCMB 0834）和须癣毛癣菌（RCMB 0925）。
方法
采用琼脂孔扩散法评估抗菌活性，并与作为抗菌参考药物的氨苄西林和庆大霉素以及作为抗真菌参考药物的两性霉素B进行比较。使用肉汤双倍稀释技术测定最低抑菌浓度（MIC）。
结果
以氨苄西林、庆大霉素和两性霉素B作为标准参考药物，报告了测试化合物的MIC值，单位为μg/mL。所得结果表明，化合物3、4、7、8、9、10、11、14、17、18、19、20和21对六种细菌和六种真菌菌株表现出显著的抗菌活性。
结论
这些有前景的化合物可作为构建具有更强抗菌作用的新衍生物的有用骨架。
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