Saravanan Govindaraj, Alagarsamy Veerachamy, Dineshkumar Pandurangan
Medicinal Chemistry Research Laboratory, Bapatla College of Pharmacy, Bapatla, Andhra Pradesh, India.
Medicinal Chemistry Research Laboratory, M.N.R. College of Pharmacy, Sangareddy, Andhra Pradesh, India.
Arch Pharm Res. 2021 Aug;44(8):1-11. doi: 10.1007/s12272-013-0262-8. Epub 2013 Oct 24.
A series of novel isoxazole coupled quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR, H NMR, mass spectroscopy and bases of elemental analysis with the aim of developing potent analgesic, anti-inflammatory and antimicrobial agents. Tail-flick technique, carrageenan-induced foot paw edema test and agar streak dilution test were performed for screening analgesic, anti-inflammatory and in vitro antimicrobial activity respectively. Moreover all compounds were examined for its ulcerogenicity. Results revealed that entire series of compounds exhibited mild to good analgesic, anti-inflammatory and antimicrobial activity with low to moderate ulcer index. The relationship between the functional group variation and the biological activity of the evaluated compounds was discussed. Out of various synthesized compounds, 2-methyl-3-(4-(5-(4-(trifluoromethyl)phenyl) isoxazol-3-yl)phenyl)quinazolin-4(3H)-one 5e was found to be the most active compound.
合成了一系列新型异恶唑偶联喹唑啉-4(3H)-酮衍生物，并通过傅里叶变换红外光谱(FT-IR)、核磁共振氢谱(¹H NMR)、质谱和元素分析进行了表征，旨在开发强效镇痛、抗炎和抗菌药物。分别采用甩尾法、角叉菜胶致足跖肿胀试验和琼脂平板稀释法筛选镇痛、抗炎和体外抗菌活性。此外，还对所有化合物进行了致溃疡作用检测。结果表明，该系列化合物均表现出轻度至良好的镇痛、抗炎和抗菌活性，溃疡指数低至中等。讨论了官能团变化与所评估化合物生物活性之间的关系。在各种合成化合物中，2-甲基-3-(4-(5-(4-(三氟甲基)phenyl)异恶唑-3-yl)phenyl)喹唑啉-4(3H)-one 5e被发现是活性最高的化合物。
