Design, synthesis, characterization and biological evaluation of some novel 1, 3, 4 oxadiazole derivatives as anti-tubercular agents targeting L, D transpeptidase 2

Abstract

Tuberculosis is a major disease causing 1.8 million deaths worldwide, every year. It represents the leading cause of mortality resulting from a bacterial infection. This point to an urgent need for new promising drug candidates to combat the drug resistance and control the disease. Recent studies reveal the ability of 1, 3, 4 Oxadiazole derivatives to produce antibacterial, anti-tubercular anticancer and anti-inflammatory activity. In the present research work a series of 4-(1, 3, 4-Oxadiazol-2-yl) pyridine based 1, 3, 4 Oxadiazole derivatives were designed and docked against Mtb enzyme target L, d transpeptidase 2. The selected molecules were synthesized and repeatedly recrystallized to attain 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. The experimental results showed that Compounds SA, VS4 and VS5 possesses anti-tubercular activity in the range of 12.5mcg/mL while Compounds VS1 and VS2 showed antitubercular activity with an MIC value of 6.25mcg/mL and compound NA exhibited moderate activity.