Department of Pharmaceutical Chemistry, King Saud University, Riyadh, Saudi Arabia.
J Pharm Pharmacol. 2013 Jun;65(6):790-7. doi: 10.1111/jphp.12039. Epub 2013 Mar 25.
The aim of this research was to study and evaluate the antimicrobial activity of a novel 2-methylsulfanyl-[1,2,4]triazolo[1,5-a]quinazoline and its derivatives. Antibacterial activity of the target compounds was tested against a variety of species of Gram-positive bacteria such as Staphylococcus aureus ATCC 29213, Bacillus subtilis ATCC6633, and Gram-negative bacteria such as Pseudomonas aeruginosa ATCC27953 and Escherichia coli ATCC 25922. In addition some yeast and fungi, Candida albicans NRRL Y-477 and Aspergillus niger, respectively, were screened.
Antimicrobial tests were carried out by the agar well diffusion method, using 100 μl of suspension containing 1 × 10(8) CFU/ml of pathological tested bacteria, 1 × 10(6) CFU/ml of yeast, and 1 × 10(4) spore/ml of fungi spread on nutrient agar (NA), Sabourand dextrose agar (SDA), and potato dextrose agar (PDA), respectively.
The minimum inhibitory concentration (MIC) of the tested compounds was determined using the broth double dilution method (serially diluted technique) in proper nutrient. For comparison, ciprofloxacin and ketoconazole were used as antibacterial and antifungal reference drugs, respectively. Compounds 6, 9, 13, 14, and 11 were found to have the highest broad-spectrum antibacterial activity against S. aureus ATCC 29213, B. subtilis ATCC6633 and Gram-negative bacteria such as P. aeruginosa ATCC27953 and E. coli ATCC 25922 with MIC values of 6.25 and 12.50 μg/ml.
It was clear that many of the synthesized compounds exhibited good antimicrobial activity. This study has revealed that compounds 6, 9, 13, 14, and 11 have been disclosed as moderate antimicrobial agents. These compounds could be useful as templates for further development through modification or derivatization to design more potent antimicrobial agents.
本研究旨在研究和评估新型 2-甲硫基-[1,2,4]三唑并[1,5-a]喹唑啉及其衍生物的抗菌活性。目标化合物的抗菌活性通过琼脂孔扩散法进行测试，针对多种革兰氏阳性菌，如金黄色葡萄球菌 ATCC 29213、枯草芽孢杆菌 ATCC6633，以及革兰氏阴性菌，如铜绿假单胞菌 ATCC27953 和大肠杆菌 ATCC 25922。此外，还筛选了一些酵母和真菌，分别为白色念珠菌 NRRL Y-477 和黑曲霉。
抗菌试验采用琼脂孔扩散法，用 100μl 含 1×10(8)个 CFU/ml 致病性测试细菌、1×10(6)个 CFU/ml 酵母和 1×10(4)个孢子/ml 真菌的悬浮液分别在营养琼脂（NA）、沙氏葡萄糖琼脂（SDA）和土豆葡萄糖琼脂（PDA）上展开。
使用肉汤双稀释法（系列稀释技术）在适当的营养物中确定了测试化合物的最小抑菌浓度（MIC）。为了进行比较，环丙沙星和酮康唑分别用作抗菌和抗真菌参考药物。化合物 6、9、13、14 和 11 被发现对金黄色葡萄球菌 ATCC 29213、枯草芽孢杆菌 ATCC6633 和革兰氏阴性菌如铜绿假单胞菌 ATCC27953 和大肠杆菌 ATCC 25922 具有最高的广谱抗菌活性，MIC 值分别为 6.25 和 12.50μg/ml。
显然，许多合成化合物表现出良好的抗菌活性。本研究表明，化合物 6、9、13、14 和 11 已被披露为中等抗菌剂。这些化合物可作为模板，通过修饰或衍生化进一步开发，设计出更有效的抗菌剂。
