SYNTHESIS, CHARACTERISATION, BIOLOGICAL EVALUATION, MTT ASSAY OF SOME NOVEL THIADIAZOLE DERIVATIVES AS ANTI-TUBERCULAR AGENTS TARGETING DECAPRENYL PHOSPHORYL BETA-D-RIBOSE2’ EPIMERASE-1

Objective: The present study was designed for the synthesis, characterization, biological evaluation, and MTT assay of some novel thiadiazole derivatives as anti-tubercular agents targeting decaprenylphosphoryl beta-d-ribose2’ epimerase-1(DPRE₁). Methods: The molecular docking study for titled compounds was performed from Autodock 4.2. Software http://autodock.scripps.edu/, pdb file was generated by chem3D.pro software tool. The binding pose for the significant compounds was visualized by Biovia, the Discovery studio visualizer. The selected molecules were synthesized and recrystallized several times to reach the expected purity. All the purified compounds were characterized by various spectral analytical techniques and evaluated for anti-mycobacterial activity against tuberculosis H37RV strain by Microplate Alamar Blue Assay (MABA) method and cell line studies. Results: The experimental results showed that the Compounds SDK3 and SDK5 have an anti-tubercular activity in the Concentration of 3.12µg/mL. Cell line studies for proprietary compounds have been carried out by MTT assay using HEK (Human embryonic kidney cells) method. It also correlated with the highest docking score. Conclusion: The development of the SDK3 and SDK5 structures will produce molecules having better anti-mycobacterial activity.