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

被引:9
作者
Eze, Florence Uchenna [1 ]
Okoro, Uchechukwu Chris [1 ]
Ugwu, David Izuchukwu [1 ]
Okafor, Sunday N. [2 ]
机构
[1] Univ Nigeria, Dept Pure & Ind Chem, Nsukka, Nigeria
[2] Univ Nigeria, Dept Pharmaceut & Med Chem, Nsukka, Nigeria
关键词
Antimicrobial; Antioxidant; Anti-inflammatory; Sulphonamide; Carboxamide; STROKE RISK; NSAIDS;
D O I
10.1016/j.bioorg.2019.103265
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 (IC50 0.3052 mg/mL) had comparable activity with Vitamin C (IC50, 0.2090 mg/mL) in the antioxidant assay.
引用
收藏
页数:10
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