New carboxamides bearing benzenesulphonamides: Synthesis,molecular docking and pharmacological properties |
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| Institution: | 1. Department of Chemistry, Visvesvaraya National Institute of Technology, Nagpur 440010, Maharashtra, India;2. Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Kingdom of Saudi Arabia;3. Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, South Africa;4. Department of Pharmaceutical Sciences, College of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia;5. Institute for Stem Cell Biology and Regenerative Medicine, NCBS, TIFR, GKVK, Bellary Road, Bangalore 560 065, India |
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| 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. |
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| Keywords: | Antimicrobial Antioxidant Anti-inflammatory Sulphonamide Carboxamide |
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