An article , which mentions Application In Synthesis of 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid, molecular formula is C6H7NO3S2. The compound – 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid played an important role in people’s production and life., Application In Synthesis of 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid
Structure-Guided Design of Thiazolidine Derivatives as Mycobacterium tuberculosis Pantothenate Synthetase Inhibitors
The pantothenate biosynthetic pathway is essential for the persistent growth and virulence of Mycobacterium tuberculosis (Mtb) and one of the enzymes in the pathway, pantothenate synthetase (PS, EC: 6.3.2.1), encoded by the panC gene, has become an appropriate target for new therapeutics to treat tuberculosis. Herein, we report nanomolar thiazolidine inhibitors of MtbPS developed by a rational inhibitor design approach. The thiazolidine compounds were discovered by using energy-based pharmacophore modelling and subsequent in vitro screening, which resulted in compounds with a half maximal inhibitory concentration (IC50) value of (1.12±0.12)muM. These compounds were subsequently optimised by a combination of modelling and synthetic chemistry. Hit expansion of the lead by chemical synthesis led to an improved inhibitor with an IC50 value of 350nM and an Mtb minimum inhibitory concentration (MIC) of 1.55muM. Some of these compounds also showed good activity against dormant Mtb cells.
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Quinuclidine – Wikipedia,
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