Plumbagin analogs-synthesis, characterization, and antitubercular activity

Abstract

Considering the emerging problem of drug resistance in tuberculosis, there is an urgent need of development of new analogs that are useful in curing drug resistant tuberculosis. In India, tuberculosis continues to remain one of the most pressing health problems. India is the highest tuberculosis burden country in the world, accounting one fifth of global incidence - estimated 2.0-2.5 million cases annually. In 2011, approximately 8.7 million new cases of tuberculosis and 1.4 million people die from tuberculosis each year worldwide. Current antitubercular therapies are successful against normal tuberculosis but it is not suitable for drug resistant tuberculosis. In this study Plumbagin analogs, obtained from Plumbago zeylanica (Family-Plumbaginaceae), have been synthesized. Out of the various synthesized analogs, the antitubercular activity of compound a and b was evaluated using standard H 37 Rv and S, H, R, and E sensitive M tuberculosis strains using LRF assay method. Compound a showed strong activity against both standard H 37 Rv and S, H, R and E sensitive M. tuberculosis strains as compared to standard Rifampicin. The other compounds are proved to be more active against standard H 37 Rv and S, H, R and E sensitive M. tuberculosis strain as compared to Rifampicin.

Keywords

• Ethambutol (R)
• isoniazid (h)
• plumbagin
• rifampicin (r)