ABSTRACT:
Tuberculosis is one of the most common deaths in the developing world. According to the world health organization, it kills more than ten lakh people annually. Numerous drugs are available for treating tuberculosis, but challenges still exist due to resistance to the present drugs available. Keeping this in view, there is a need to develop a new antitubercular agent. In the present study, a series of benzimidazole thiadiazolyl azetidinone derivatives 5(a-h) were designed and synthesized using multiple steps. In the first step, using multiple steps, benzo imidazolyl acetate was prepared and converted to benzylidene benzo imidazolyl thiadiazol amine derivatives 4(a-h) intermediate. In the final step benzimidazole thiadiazolyl azetidinone derivatives 5(a-h) were prepared. All these synthesized compounds were confirmed using IR, 1H NMR, and mass spectral data. Further, the physiochemical properties of these compounds 5(a-h) and interaction pattern to receptor (PDB Code: 4COD) were studied using the Insilco method. Compounds 5(a-h) were evaluated for anti-tubercular activity against M. tuberculosis H37Rv using Microplate Alamar Blue Assay and compared with the standard drug isoniazid. Among all these compounds, 5b showed the best anti-tubercular activity with a MIC value of 3.12µg/ml. The docking score ranged from -2.13 to -5.07kcal/mol, and physiochemical properties were within prescribed limits. The anti-tubercular results of most compounds were promising, and among all compounds, 5b showed the best result, which can be further evaluated by in vivo studies.