Synthesis and biological evaluation of propargyl acetate derivatives as anti-mycobacterial agents

This study is focused on propargyl acetate derivatives. Eight molecules were designed based on propargyl alcohols and different acid anhydrides.All the synthesized compounds and commercially available ones were evaluated for anti-tuberculosis activity.Inhibitors against Mtb have been identified and characterized for further development into potential novel anti-tubercular drugs.Tuberculosis (TB) is a deadly infectious disease and is the leading cause of death worldwide, killing around 2 million people annually, primarily in developing countries. The World Health Organization (WHO) estimates that over one third of the world’s population is infected with TB with approximately 8 million new cases of infection diagnosed every year [1-3]. After human immunodeficiency virus (HIV)/AIDS, TB is the second most common cause of death due to an infectious disease, and current trends suggest that TB will still be among the 10 leading causes of global disease burden in the year 2020 [4]. TB incidence is also on the rise because of the correspondingly high HIV infection rates. These two diseases progress at faster rates in co-infected individuals. The immune systems have been compromised by HIV/AIDS, so individuals fall victims to TB which takes opportunity of their weakened immune systems. There is a great interest in the scientific field to come up with a new drug(s) to combat TB. Tuberculosis is an airborne infectious disease caused by mycobacteria, mainly Mycobacterium tuberculosis (Mtb) [5]. The success of mycobacteria in producing disease relies entirely on its ability to utilize macrophages for its replication and more importantly, the maintenance of viability of host macrophages that sustain mycobacteria.In the present scenario, due to the emergence of multi-drug resistant tuberculosis (MDR-TB) and association between HIV and TB, Directly Observed Treatment Short course (DOTS) is becoming rapidly ineffective in controlling tuberculosis. Recent reports indicate that, areas