Antibacterial, Antioxidant and DNA Cleavage Activity Evaluation of Substituted Phenylureido Sulfaguanidine and Sulfamethazine Derivatives

A series of six N -carbamimidoyl-4-(3-substituted phenylureido) benzenesulfonamides ( SG1-SG6 ) and six N-(4,6-dimethylpyrimidin-2-yl)-4-(3-substituted phenylureido) benzenesulfonamides ( SM1-SM6 ) were successfully re-synthesized to determine their antibacterial, antioxidant, and DNA cleavage activ...

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Veröffentlicht in:Pharmaceutical chemistry journal 2022-06, Vol.56 (3), p.345-349
Hauptverfasser: Tekeli, Yener, Lolak, Nebih, Sonmez, Gorkem Deniz, Tekeli, Tuba, Akocak, Suleyman
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Sprache:eng
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Zusammenfassung:A series of six N -carbamimidoyl-4-(3-substituted phenylureido) benzenesulfonamides ( SG1-SG6 ) and six N-(4,6-dimethylpyrimidin-2-yl)-4-(3-substituted phenylureido) benzenesulfonamides ( SM1-SM6 ) were successfully re-synthesized to determine their antibacterial, antioxidant, and DNA cleavage activities. In general, all compounds showed moderate to good activity against Gram-positive strains ( S. aureus and E. faecalis ) and Gram-negative strains ( P. aeruginosa and E. coli) . More specifically, compound SM6 showed great potency against all the tested bacterial strains. One compound ( SM5 ) among the series tested, showed great potency against P. aeruginosa strain (minimal inhibitory concentration, MIC = 7.8 μg/mL), which was comparable with MICs of the standard drugs ampicillin and ceftriaxon (3.9 and 15.6 μg/mL, respectively). On the other hand, a weak antioxidant activity was observed using DPPH free radical scavenging assay. Taken together, several compounds from the current series might be interesting lead derivatives to develop more potent compounds against the test bacterial strains.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-022-02654-7