Journal article Open Access

NOVEL COMPOUNDS OF THIO-PYRIMIDINE ANTHRANILATE AND SULFONAMIDE ANTHRANILATE DERIVATIVES WITH ANTIMICROBIAL ACTIVITY AND IT'S SYNTHESIS

Nitin A. Shimpi*, Rajesh B. Dhake

Sulfonamide and Thio-pyrimidines derivatives are known for antibacterial activity and hence, in our research study, series of compounds were designed for the Thio-pyrimidine anthranilate and Sulphonamide anthranilate derivatives. Based on the N-terminal signal peptidase and C-terminal sorting signal of surface protein binding, Compound-1.4 (S-Allyl-Methyl ester), Compound 2.2 (S-Allyl-Amino-Acid), Compound-3.1 (Methyl-ester-Methyl-sulfonamide) & Compound-4.1 (Methyl-ester-Toluene-sulfonamide) were selected for our research as these compounds shown advantage in the binding. These four compounds were synthesized by chemical synthesis and characterized using structure elucidating techniques like NMR and Mass spectroscopy. These compounds were screened for the biological activity using Gram positive (Bacillus subtilis, Staphylococcus aureus) and Gram negative bacteria (Escherichia coli and Klebsiella Pneumoniae). In vitro Antibacterial Assay (Table-1) indicates that all the synthesized compounds (1.4, 2.2, 3.1 & 4.1) shows moderate to excellent activity data against all the tested Gram positive as well as Gram negative bacterial pathogens determined at concentration 10, 50, 100 and 200 μg/mL. From the activity data, it is concluded that the compound 2.2 & 4.1 are most active among all the tested compounds for the tested bacterial species, while compound 3.1 shows comparable activity compared to Chloramphenicol and Ciprofloxacin.

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