Diarylcoumarins inhibit mycolic acid biosynthesis and …
Tuberculosis (TB) is one of the world's deadliest diseases (). The Centers for Disease Control and Prevention has reported that each year, eight million people around the world become sick with TB and there are over two million TB-related deaths worldwide. Moreover, one-third of the world's population is infected with TB. Thus, Mycobacterium tuberculosis (the causative agent of TB) is clearly the most predominant global human pathogen. Two decades ago, it was thought that TB was under control and that it was a matter of time before it would be eradicated. Today, this disease has reestablished itself due to several factors. The lack of drug compliance, the appearance of multiple-drug-resistant strains, and the AIDS epidemic are a few factors that have led to the resurgence in TB. Drug resistance arises following inadequate compliance, and AIDS patients with weakened immune system are very susceptible to M. tuberculosis and the usual cause of death.
LanéelleThe biosynthesis of mycolic acids by ..
Mycolic acid; Mycobacterium tuberculosis ..
(iii) Mycolic acid synthesis is the target of well-known antituberculosis drugs, i.e., isoniazid, ethionamide, and thiocarlide (). This suggests that all reactions on the pathway to synthesis and processing of mycolic acids are viable targets for new drug discovery (target validation).
Mycolic acid biosynthesis and ..
(ii) Deletion of the proximal cyclopropane ring of α-mycolate or deletion of the methoxy- and keto-mycolates leads to a significant attenuation of growth of the two mutants in the mouse model of infection. Deletion of keto-mycolates in M. tuberculosis leads to restricted growth of this mutant in macrophages. Thus, the distribution and fine structure of mycolic acids determine the virulence of M. tuberculosis. It can be concluded that mycolic acids are very important components of the pathogenic M. tuberculosis.