JOURNAL OF PHARMACOLOGY AND
BIOMEDICINE
ISSN.2456-8244
In the present study, a series of novel sydnone-based derivatives (ASa-e) incorporating chalcone and substituted arylamide/morpholine moieties were synthesized and evaluated for their antibacterial activity and pharmacokinetic characteristics. The target compounds were synthesized through a multi-step reaction sequence and characterized by physicochemical parameters, thin-layer chromatography (TLC), Fourier-transform infrared (FTIR) spectroscopy, and 1H NMR spectroscopy. Antibacterial activity was assessed against Escherichia coli and Staphylococcus aureus using the agar well diffusion method at concentrations ranging from 25 to 100 μg/mL. All synthesized compounds exhibited concentration-dependent antibacterial activity, with the halogen-substituted derivatives showing superior efficacy compared to non-halogenated analogues. Among the tested compounds, ASd, containing a bromo-substituted phenyl group, demonstrated the highest antibacterial activity, producing inhibition zones of up to 19 mm against E. coli and 16 mm against S. aureus. In silico ADMET and physicochemical assessments revealed that all compounds complied with Lipinski’s rule of five, possessed acceptable bioavailability profiles, and exhibited favorable pharmacokinetic characteristics. The findings suggest that sydnone-chalcone hybrids, particularly halogenated derivatives, represent promising lead molecules for the development of new antibacterial agents and warrant further biological investigation.
NAMES:
ONLINE ISSN:24568244
Keywords: Sydnone, chalcone, anti-bacterial, mesoionic, in-silico
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