Antitubercular agent-32 

Antitubercular agent-32 is a derivate of Benzothiazinone (HY-13579A), inhibits M. tuberculosis, and shows improved metabolic stability and enhanced water solubility. Antitubercular agent-32 exerts antitubercular effect by targeting decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, IC₅₀=3.9 μM)^[1].

Antitubercular agent-32 (compound 8) (0-7.5 mg/mL; 48 h) shows low cytotoxicity and inhibits M. tuberculosis H37Rv with the minimum inhibition concentration (MIC) of 40 nM^[1].
Antitubercular agent-32 (0-20 μM) inhibits decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, 0.5 μM), an enzyme essential for the biosynthesis of mycobacterial cell wall, with an IC₅₀ value of 3.9 μM^[1].
Antitubercular agent-32 (1 μM; 10 min) exhibits metabolic stability in the liver microsomal metabolic of both human (HLM) and mouse (MLM), with fast clearance rates of 77 mL/min/kg (HLM) and 163 mL/min/kg (MLM), respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

492.61

C₂₂H₂₈N₄O₅S₂

2498762-42-6

CS(=O)(C(C=C12)=CC([N+]([O-])=O)=C1SC(N(CCN3CC4CCCCC4)CC53CC5)=NC2=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Shi R, et al. Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents. ACS Med Chem Lett. 2022 Mar 10;13(4):593-598.   [Content Brief]