Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2452, Riyadh 11495, Saudi Arabia; Department of Pharmacognosy, Faculty of Pharmacy, Helwan University, Cairo 11795, Egypt.
Microb Pathog. 2018 Apr;117:60-67. doi: 10.1016/j.micpath.2018.02.018. Epub 2018 Feb 9.
Previously, seventeen 2-phenoxy-benzo[g][1,2,4]triazolo[1,5-a]quinazoline derivatives were prepared and characterized by physicochemical and spectral means. This study was conducted to evaluate their activities in vitro against five Gram-negative and five Gram-positive of clinically pathogenic bacterial strains and ten fungal strains. The antimicrobial activity was assessed, and the minimum inhibitory concentration values of the tested compounds were determined in μg ml, using the diffusion agar technique. The bacterial strains used were Escherichia coli (ATCC 25922), Proteus mirabilis (ATCC 7002), Klebsiella oxytoca (ATCC 700324), Pseudomonas aeruginosa (ATCC 10145), Enterobacter cloacae (ATCC 13047D-5), Bacillus subtilis (NRRL B-543), Enterococcus faecalis (RCMB 0100154-2), Staphylococcus aureus (ATCC 29213), Staphylococcus epidermidis (ATCC 12228), and Streptococcus pyogenes (RCMB 0100174-2). Aspergillus fumigatus (RCMB 02568), Syncephalastrum racemosum (IMI 21178), Geotricum candidum (IMI 329542), Candida albicans (ATCC 10231), Aspergillus niger (IMI 130783), Cryptococcus neoformans (NRRL Y-1518), Candida tropicalis (RCMB 05239), Penicillium expansum (IMI 146655), Microsporum canis (RCMB 0834), and Trichophyton mentagrophytes (RCMB 0925) were used as the fungal strains. Ampicillin and gentamicin were used as reference antibacterial drugs and amphotericin B was used as the reference antifungal drug. The antimicrobial studies revealed that the tested compounds 6-8, 11, 12, and 14-16 showed the highest activities against the bacterial and fungal strains. The current study showed that some benzo[g]traizoloquinazolines displayed remarkable antimicrobial activity and could be used as template for further design of potent antimicrobial agent.
先前，通过物理化学和光谱手段，制备并表征了十七种 2-苯氧基苯并[g][1,2,4]三唑并[1,5-a]喹唑啉衍生物。本研究旨在评估它们对五种临床致病性革兰氏阴性和革兰氏阳性细菌菌株以及十种真菌菌株的体外活性。采用琼脂扩散技术，评估了抗菌活性，并测定了测试化合物的最小抑菌浓度值（μg/ml）。所用的细菌菌株为大肠杆菌（ATCC 25922）、奇异变形杆菌（ATCC 7002）、产酸克雷伯菌（ATCC 700324）、铜绿假单胞菌（ATCC 10145）、阴沟肠杆菌（ATCC 13047D-5）、枯草芽孢杆菌（NRRL B-543）、粪肠球菌（RCMB 0100154-2）、金黄色葡萄球菌（ATCC 29213）、表皮葡萄球菌（ATCC 12228）和化脓性链球菌（RCMB 0100174-2）。烟曲霉（RCMB 02568）、丛赤壳（IMI 21178）、近平滑念珠菌（IMI 329542）、白色念珠菌（ATCC 10231）、黑曲霉（IMI 130783）、新生隐球菌（NRRL Y-1518）、热带念珠菌（RCMB 05239）、扩展青霉（IMI 146655）、犬小孢子菌（RCMB 0834）和须癣毛癣菌（RCMB 0925）被用作真菌菌株。氨苄西林和庆大霉素被用作参考抗菌药物，两性霉素 B 被用作参考抗真菌药物。抗菌研究表明，测试化合物 6-8、11、12 和 14-16 对细菌和真菌菌株表现出最高的活性。本研究表明，一些苯并[g]三唑并喹唑啉显示出显著的抗菌活性，可作为进一步设计有效抗菌剂的模板。
