Authors Kovalenko, OP; Volynets, GP; Rybak, MY; Starosyla, SA; Gudzera, OI; Lukashov, SS; Bdzhola, VG; Yarmoluk, SM; Boshoff, HI; Tukalo, MA in ROYAL SOC CHEMISTRY published article about ANTIBACTERIAL ACTIVITY; QUALITY-CONTROL; TUBERCULOSIS; DISCOVERY; DESIGN in [Kovalenko, Oksana P.; Rybak, Mariia Yu; Gudzera, Olga, I; Tukalo, Michael A.] NAS Ukraine, Inst Mol Biol & Genet, Dept Prot Synth Enzymol, 150 Zabolotnogo 54, UA-03143 Kiev, Ukraine; [Volynets, Galyna P.; Starosyla, Sergiy A.; Lukashov, Sergiy S.; Bdzhola, Volodymyr G.; Yarmoluk, Sergiy M.] NAS Ukraine, Inst Mol Biol & Genet, Dept Med Chem, 150 Zabolotnogo 54, UA-03143 Kiev, Ukraine; [Boshoff, Helena, I] NIAID, TB Res Sect, Lab Clin Immunol & Microbiol, NIH, 5601 Fishers Lane,MSC 9806, Bethesda, MD 20892 USA in 2019.0, Cited 38.0. SDS of cas: 93-02-7. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7
Effective treatment of tuberculosis is challenged by the rapid development of Mycobacterium tuberculosis (Mtb) multidrug resistance that presumably could be overcome with novel multi-target drugs. Aminoacyl-tRNA synthetases (AARSs) are an essential part of protein biosynthesis machinery and attractive targets for drug discovery. Here, we experimentally verify a hypothesis of simultaneous targeting of structurally related AARSs by a single inhibitor. We previously identified a new class of mycobacterial leucyl-tRNA synthetase inhibitors, N-benzylidene-N ‘-thiazol-2-yl-hydrazines. Molecular docking of a library of novel N-benzylidene-N ‘-thiazol-2-yl-hydrazine derivatives into active sites of M. tuberculosis LeuRS (MtbLeuRS) and MetRS (MtbMetRS) resulted in a panel of the best ranking compounds, which were then evaluated for enzymatic potency. Screening data revealed 11 compounds active against MtbLeuRS and 28 compounds active against MtbMetRS. The hit compounds display dual inhibitory potency as demonstrated by IC50 values for both enzymes. Compound 3 is active against Mtb H37Rv cells in in vitro bioassays.
SDS of cas: 93-02-7. Welcome to talk about 93-02-7, If you have any questions, you can contact Kovalenko, OP; Volynets, GP; Rybak, MY; Starosyla, SA; Gudzera, OI; Lukashov, SS; Bdzhola, VG; Yarmoluk, SM; Boshoff, HI; Tukalo, MA or send Email.
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