DOI:

Synthesis, structure elucidation and antibacterial screening of some novel 1,3,4-oxadiazoline derivatives



Arshad, Mohammad ; Beg, Md Amjad; Bhat, Abdul R; Athar, Fareeda

Abstract

Anovel sequence of 1,3,4-oxadiazoline derivatives has been synthesized with an endeavour to explore their consequence on in vitro growth of microbes causing the microbial contagion. In vitro antimicrobial activity has been performed against the Escherichia coli (E. coli) and Proteus mirabilis (P. mirabilis) which are Gram-negative (Gram-ve) and Staphylococcus aureus (S. aureus) and Staphylococcus epidermidis (S. epidermis) which are Gram-positive (Gram+ve) by using disk diffusion method. The minimum inhibitory concentration (MIC) has been distinguished by employing the double dilution method. The result of percent inhibition area/µg of the compounds has been differentiated with the standard drug “Ciprofloxacin”. Several compounds portray excellent activity as compared to the standard drug Ciprofloxacin while some of them presented a considerable zone of inhibition. The evaluated compounds for cytotoxicity effects via Human hepatocellular carcinoma (HepG2) cell line by MTT-assay and findings reveal that the experimental compounds display a viability of ≥80% at 100 µM. In molecular docking studies, the 1,3,4-oxadiazoline derivatives demonstrate the ligand-receptor interaction with amino acids which exist on the active sites of the peptide deformylase and the 1,3,4-oxadiazoline derivatives exhibit their antibacterial potential as peptide deformylase inhibitors.

 


Keyword(s)

Synthesis, 1,3,4-oxadiazoline, antimicrobial activity, MTT-assay

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