Bulletin of the Chemical Society of Ethiopia · 2018 · 22 citations · 9 references
PharmacyMedicinal ChemistryMicrobiologyDrug DiscoveryStructure-activity RelationshipsSynthetic Medicinal ChemistryAntifungal AgentsStructure-activity Relationship AnalysisAmine BasesAntimicrobial Drug DevelopmentAntioxidant Activity AssaysNew Antifungal AgentsNovel Antibacterial Drug DiscoveryNucleophilic Acyl SubstitutionNucleophilic Aliphatic SubstitutionStructural Elucidation From Spectra
Five novel sulfonamides derivatives HR5-HR8 and HR14 were synthesized by sulfonylation of primary or secondary amine in the presence of base through nucleophilic substitution reaction. Structural elucidation was carried out through FT-IR, UV, 1H NMR, MS and elemental analysis. Prepared compounds were evaluated against pathogenic strains of bacteria (S. aureus and E. coli) and fungi (A. flavous and A. nyger). Results were compared against standard antifungal and bacterial drug already available in market (isoconazole and sulfmethoxazole). It was found that compound HR14 showed good activity with MIC 1.5 µg/mL and 2.0 µg/mL for S. aurues and E. coli, respectively. While HR5 showed best antifungal activity with zone of inhibition 27.2+0.12 mm (MIC: 5.25 µg/mL) and 18.1+0.12 mm (MIC: 12.5 µg/mL) against A. flavous and A. nyger, respectively. Synthesized compounds were also tested for their in vitro antioxidant activity by using DDPH. Amongst all compounds HR5 was found to have potential activity with 15.60% antioxidant activity at 6 mM concentration. KEY WORDS: Sulfonamide, DPPH, AntiMICrobial activity Bull. Chem. Soc. Ethiop. 2017, 31(3), 491-498.DOI: http://dx.doi.org/10.4314/bcse.v31i3.13
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Iraj Rahavi Ezabadi, Charalabos Camoutsis, Panagiotis Zoumpoulakis et al. · Bioorganic & Medicinal Chemistry · 2007 · 235 citations
S. Stokes, Robert Albert, Ed T. Buurman et al. · Bioorganic & Medicinal Chemistry Letters · 2012 · 87 citations