A New Class of Antimycobacterial Agent that Kills TB Bugs

A New Class of Antimycobacterial Agent


Report that was originally published in Science Express on 19 March 2009 & Science 8 May 2009:Vol. 324. no. 5928, pp. 801 - 804 is really highly helpful in the area of TB research where new drugs are required to counter the tuberculosis (TB) pandemic (Source:www.sciencemag.org). In this report, Dr. Stewart T. Cole1 and co-workers working in different institutes, etc.(contact address: stewart.cole@epfl.ch) have described the synthesis and characterization of 1,3-benzothiazin-4-ones (BTZs), a new class of antimycobacterial agents that kill Mycobacterium tuberculosis in vitro, ex vivo, and in mouse models of TB.

Using genetics and biochemistry, they have identified the enzyme decaprenylphosphoryl-β-D-ribose 2'-epimerase as a major BTZ target. Inhibition of this enzymatic activity abolishes the formation of decaprenylphosphoryl arabinose, a key precursor that is required for the synthesis of the cell-wall arabinans, thus provoking cell lysis and bacterial death. The most advanced compound, BTZ043, is a candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant TB.