Murti Y, Singh A K, Pathak D
Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura-281 001, India.
Indian J Pharm Sci. 2011 May;73(3):333-7. doi: 10.4103/0250-474X.93512.
New quinazolin-4-one derivatives, 6-bromo-2-methyl-3-(substituted phenyl)-(3H)-quinazolin-4-one, were synthesized and evaluated for antimicrobial and antiinflammatory activities. The structures attributed to synthesized compounds 1-8 were supported by the results of elemental analysis as well as by the UV, IR and (1)H NMR spectral data. Investigation of antimicrobial activity was performed using cup-plate agar diffusion method against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa and Candida albicans, Aspergillus niger and Curvularia lunata. Antiinflammatory activity was evaluated using the carrageenan-induced paw oedema test in rats. The results showed that compounds 2b, 2c, 2d, 2g and 2h exhibited significant antibacterial and antifungal activity comparable to standard drugs and compounds 2b and 2c showed good antiinflammatory activity comparable to ibuprofen.
合成了新型喹唑啉-4-酮衍生物6-溴-2-甲基-3-(取代苯基)-(3H)-喹唑啉-4-酮，并对其抗菌和抗炎活性进行了评估。通过元素分析结果以及紫外、红外和(1)H核磁共振光谱数据，证实了所合成化合物1-8的结构。采用杯碟琼脂扩散法对枯草芽孢杆菌、金黄色葡萄球菌、铜绿假单胞菌、白色念珠菌、黑曲霉和新月弯孢霉进行抗菌活性研究。采用角叉菜胶诱导大鼠足趾肿胀试验评估抗炎活性。结果表明，化合物2b、2c、2d、2g和2h表现出与标准药物相当的显著抗菌和抗真菌活性，化合物2b和2c表现出与布洛芬相当的良好抗炎活性。
