Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka, Nigeria.
Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka, Nigeria.
Bioorg Chem. 2019 Nov;92:103265. doi: 10.1016/j.bioorg.2019.103265. Epub 2019 Sep 9.
Ten new derivatives of benzenesulphonamide bearing carboxamide functionality were synthesized and investigated for their in vitro antimicrobial, antioxidant and in vivo anti-inflammatory activities. Compound 9d inhibited carrageenan induced rat-paw oedema at 93.81, 88.79 and 86.09% at 1 h, 2 h and 3 h administration respectively. In the antimicrobial activity, compound 9a (6.54, 6.69 and 6.64 mg/mL) was most potent against S. aureus, B. subtilis and C. albicans respectively, compound 9e (6.45 and 6.46 mg/mL) was most active against P. aeruginosa and A. niger respectively while compound 9i (6.24 mg/mL) was most active against E. coli. Only compound 9a (IC 0.3052 mg/mL) had comparable activity with Vitamin C (IC 0.2090 mg/mL) in the antioxidant assay.
合成了十种具有羧酰胺官能团的苯磺酰胺衍生物,并研究了它们的体外抗菌、抗氧化和体内抗炎活性。化合物 9d 在 1h、2h 和 3h 给药时,分别以 93.81%、88.79%和 86.09%的抑制率抑制角叉菜胶诱导的大鼠足肿胀。在抗菌活性方面,化合物 9a(6.54、6.69 和 6.64mg/mL)对金黄色葡萄球菌、枯草芽孢杆菌和白色念珠菌的抑制作用最强,化合物 9e(6.45 和 6.46mg/mL)对铜绿假单胞菌和黑曲霉的抑制作用最强,而化合物 9i(6.24mg/mL)对大肠杆菌的抑制作用最强。只有化合物 9a(IC0.3052mg/mL)在抗氧化测定中与维生素 C(IC0.2090mg/mL)具有相当的活性。