Background:
Tuberculosis (TB) continues to be the most threatening cause of death in recent years. There is urgent need of search more potent, less toxic antitubercular agents.
Methods:
A set of five new 1,3,4-oxadiazolyl-imidazo-1,2-pyridine derivatives (4a-4e) was synthesized and screened invitro for their antibacterial activity against Mycobacterium tuberculosis (H37 RV strain) ATCC No-27294.
Results:
Compound 4b displayed potent antitubercular activity at MIC 6.25 µg/mL. In-silico molecular docking studies
were performed for evaluation of the binding patterns of compounds 4a-4e in the binding site of proteins like, Pantothenate
synthatase and enoyl acyl reductase inhibitor. The outcomes of the in- vitro antitubercular studies were in well agreement
with the molecular docking studies. These newly synthesized compounds were found to have good ADMET profile. We also explored possible anticancer activity using in-silico methods.
Conclusion:
These results shows that readily synthesized 1,3,4-oxadiazolyl-imidazo-1,2-pyridine derivatives (4a-4e) are attracting new class of potent anti-TB targets as well as possible anticancer activity that worth additional opportunities for improvements.
A new class of platinum(ii) complexes with the phosphine ligand pta which show potent anticancer activity
