Ajay Kumar
Pharmaceutical Chemistry
May 2025
This study reports the synthesis, structural characterization, and antibacterial evaluation of five novel derivatives of sulfamethoxazole, designed through targeted chemical modifications at the para-amino group to enhance antimicrobial potency. The derivatives (SMX-1 to SMX-5) were synthesized via condensation, acylation, substitution, and esterification reactions, and structurally confirmed using Fourier Transform Infrared Spectroscopy (FTIR), ¹H NMR, and mass spectrometry techniques. The antibacterial activity of the synthesised compounds was assessed in vitro using the broth microdilution and agar well diffusion procedures against Staphylococcus aureus and Escherichia coli. Among the derivatives, SMX-3 demonstrated the most potent activity with the largest inhibition zones and lowest minimum inhibitory concentrations (MIC), followed by SMX-4 and SMX-2. Efficiency scores calculated as the ratio of inhibition zone to MIC affirmed the enhanced biological performance of these derivatives compared to the parent drug and standard antibiotic. The results highlight the potential of rational structural derivatization of sulfamethoxazole in overcoming resistance and improving therapeutic efficacy.
423- 438
© Airo Journals 2021
