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新型含苯磺酰胺基的羧酰胺类化合物的合成、分子对接及药理学性质研究。

New carboxamides bearing benzenesulphonamides: Synthesis, molecular docking and pharmacological properties.

机构信息

Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka, Nigeria.

Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka, Nigeria.

出版信息

Bioorg Chem. 2019 Nov;92:103265. doi: 10.1016/j.bioorg.2019.103265. Epub 2019 Sep 9.

Abstract

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.

摘要

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。

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