http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis
Makarov, V.,Manina, G.,Mikusova, K.,Mollmann, U.,Ryabova, O.,Saint-Joanis, B.,Dhar, N.,Pasca, M. R.,Buroni, S.,Lucarelli, A. P.,Milano, A.,De Rossi, E.,Belanova, M.,Bobovska, A.,Dianiskova, P.,Kordula American Association for the Advancement of Scienc 2009 Science Vol.324 No.5928
<P>New drugs are required to counter the tuberculosis (TB) pandemic. Here, we describe 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, we identified the enzyme decaprenylphosphoryl-beta-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.</P>