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- W4384203227 endingPage "1975" @default.
- W4384203227 startingPage "1975" @default.
- W4384203227 abstract "Tuberculosis (TB) is a leading infectious disease with serious antibiotic resistance. The benzothiazinone (BTZ) scaffold PBTZ169 kills Mycobacterium tuberculosis (Mtb) through the inhibition of the essential cell wall enzyme decaprenylphosphoryl-β-D-ribose 2'-oxidase (DprE1). PBTZ169 shows anti-TB potential in animal models and pilot clinical tests. Although highly potent, the BTZ type DprE1 inhibitors in general show extremely low aqueous solubility, which adversely affects the drug-like properties. To improve the compounds physicochemical properties, we generated a series of BTZ analogues. Several optimized compounds had MIC values against Mtb lower than 0.01 µM. The representative compound 37 displays improved solubility and bioavailability compared to the lead compound. Additionally, compound 37 shows Mtb-killing ability in an acute infection mouse model." @default.
- W4384203227 created "2023-07-14" @default.
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- W4384203227 date "2023-07-12" @default.
- W4384203227 modified "2023-10-18" @default.
- W4384203227 title "Side Chain-Modified Benzothiazinone Derivatives with Anti-Mycobacterial Activity" @default.
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- W4384203227 doi "https://doi.org/10.3390/biomedicines11071975" @default.
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