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DprE1-IN-377790 is a novel DprE1 inhibitor, killing M. tuberculosis.

DprE1-IN-2 is an effective DprE1 inhibitor.

DprE1-IN-11 (compound 3) is an orally active DprE1 inhibitor that exhibits antitubercular activity against both MTB H37Rv and MDR-MTB strains (MIC <0.029-0.095 μM).

DprE1-IN-13 (Compound 42) is an inhibitor of decaprenyl-phosphoryl-β-d-ribose oxidase (DprE1) with an IC50 value of 12.72 μM. It effectively inhibits Mycobacterium tuberculosis H37Ra, with a MIC50 of 1.071 μM.

DprE1-IN-4 is a potent, non-covalent inhibitor of DprE1 (IC50: 0.90 μg mL). DprE1-IN-4 has acceptable pharmacokinetic properties and has a significant bactericidal effect in a mouse model of acute tuberculosis.

DprE1-IN-1 is a potent, orally active DprE1 inhibitor that demonstrates good hepatocyte stability, low cytotoxicity, and low hERG channel inhibition. It also exhibits effective anti-branched bacilli activity in macrophages, reducing the bacterial load by 1.29 log10 CFU.

DprE1-IN-9 (compound B18) is an efficient, reversible inhibitor of DprE1, interacting with the enzyme's receptor cavity. It exhibits potent antimycobacterial properties, demonstrating activity against non-pathogenic H37Ra (MIC=0.18 µg mL) and pathogenic strains, including H37Rv, as well as clinical MDR and XDR isolates [1].

DprE1-IN-5 (Compound 10), a potent DprE1 inhibitor, exhibits anti-TB activity with an MIC of 4 μM against the Mtb H37Rv strain and demonstrates antimycobacterial efficacy against drug-resistant strains. Additionally, it possesses high microsomal stability [1].

DprE1-IN-6 (Compound 56) is a DprE1 inhibitor with anti-TB activity, showing a minimum inhibitory concentration (MIC) of 1 μM against the Mtb H37Rv strain and efficacy against drug-resistant mycobacterial strains. Additionally, it has high microsomal stability and medium clearance [1].

DprE1-IN-7 (Compound 64) is a DprE1 inhibitor with potent anti-tuberculosis (TB) activity, demonstrating a minimum inhibitory concentration (MIC) of 1 μM against the Mtb H37Rv strain. It exhibits antimycobacterial effects on drug-resistant strains, shows high microsomal stability, and has medium clearance [1].

DprE1-IN-8, a potent DprE1 inhibitor with an IC50 of less than 0.75 μM, demonstrates significant activity against Mtb H37Rv, with an IC50 of 6 nM, making it applicable in tuberculosis research [1].