Abstract
The compounds were tested against panel of three Gram-positive, viz. Staphylococcus aureus, Bacillus subtilis, Bacillus cereus and three Gram-negative bacterial strains viz. Pseudomonas aeruginosa, Escherichia coli, and Proteus vulgaris where they showed significant to moderate antibacterial activity. The compound also showed considerable antibiofilm activity against S.aureus and B.subtilis. The most potent compounds 7l and 7m found bacteriostatic in time-kill assay via inhibition of DNA gyrase enzyme and interacting with Glu58, Val130, Ile175 and Ile186 via numerous H-bonds as revealed by docking. In S.aureus-induced murine infection model, compound 7m showed dose-dependent reduction of viability of bacteria with maximum activity in 25mg/kg treated group. The antifungal activity against human fungal pathogens was also estimated, where these compounds showed considerable inhibitory activity as compared to standard. The metabolic liability of compound 7m was determined using RS-Predictor and MetaPrint 2D React. The molecules were proved as effective antibacterial agent via inhibition of DNA gyrase as a mechanism together with significant antifungal activity.
Highlights
The past few decades have witnessed the discovery of new antibiotics and derivatives thereof which has enhances our capacity to fight against the infectious diseases [1,2]
The compounds were tested against panel of three Gram-positive, viz. Staphylococcus aureus, Bacillus subtilis, Bacillus cereus and three Gram-negative bacterial strains viz. Pseudomonas aeruginosa, Escherichia coli, and Proteus vulgaris for determination of their antibacterial efficacy using cefixime as a standard drug
All synthesized compounds were screened for their minimum inhibitory concentration (MIC, μg⁄mL) against selected four Gram-positive, viz. Staphylococcus aureus (NCIM–2079), Bacillus subtilis (NCIM– 2063), Bacillus cereus (NCIM–2156), Staphylococcus Epidermidis and four Gram-negative bacterial strains viz. Pseudomonas aeruginosa (NCIM–2036), Escherichia coli (NCIM–2065), Proteus Mirabilis and Proteus vulgaris by the broth dilution method as recommended by the National Committee for Clinical Laboratory Standards with minor modifications [20]
Summary
The past few decades have witnessed the discovery of new antibiotics and derivatives thereof which has enhances our capacity to fight against the infectious diseases [1,2]. The compounds were tested against panel of three Gram-positive, viz. Staphylococcus aureus, Bacillus subtilis, Bacillus cereus and three Gram-negative bacterial strains viz. Pseudomonas aeruginosa, Escherichia coli, and Proteus vulgaris for determination of their antibacterial efficacy using cefixime as a standard drug. The most potent compounds 7l amd 7m found bacteriostatic in time kill assay via inhibition of DNA Gyrase enzyme.
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
