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 (IC50 0.3052 mg/mL) had comparable activity with Vitamin C (IC50 0.2090 mg/mL) in the antioxidant assay.
Keywords:
Anti-inflammatory; Antimicrobial; Antioxidant; Carboxamide; Sulphonamide.
Copyright © 2019 Elsevier Inc. All rights reserved.
MeSH terms
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Animals
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Antifungal Agents / chemical synthesis
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology*
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Antioxidants / chemical synthesis
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Antioxidants / chemistry
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Antioxidants / pharmacology*
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Aspergillus niger / drug effects
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Bacillus subtilis / drug effects
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Benzenesulfonamides
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Biphenyl Compounds / antagonists & inhibitors
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Candida albicans / drug effects
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Dose-Response Relationship, Drug
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Edema / drug therapy
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Escherichia coli / drug effects
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Male
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Molecular Docking Simulation*
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Molecular Structure
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Picrates / antagonists & inhibitors
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Pseudomonas aeruginosa / drug effects
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Rats
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Staphylococcus aureus / drug effects
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
Substances
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Anti-Bacterial Agents
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Anti-Inflammatory Agents, Non-Steroidal
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Antifungal Agents
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Antioxidants
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Biphenyl Compounds
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Picrates
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Sulfonamides
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1,1-diphenyl-2-picrylhydrazyl