dpre1

DprE1-IN-2 is an effective DprE1 inhibitor.

TBA-7371 (DprE1-IN-1) is a potent inhibitor of DprE1 and PDE6.

BTZ043 is a DprE1 inhibitor with nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.

Macozinone (PBTZ169) inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043.

BTZ043 Racemate (Benzothiazinone 10526038) is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor, used as a new antimycobacterial agent.

TCA1 (TCA 1) is a small molecule with activity against drug-resistant and persistent tuberculosis.

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-14 (Compound 77) is a DprE1 inhibitor with an IC₅₀ of 2.5 nM against M. tuberculosis. It demonstrates antitubercular activity with an MIC₉₀ of 0.3 μM against the M. tuberculosis mc²⁶²³⁰ strain. Primarily exhibiting bacteriostatic activity, DprE1-IN-14 shows time-dependent bactericidal effects at concentrations 10 times the MIC. This compound is applicable in antituberculosis research.

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-10 (hit 2), an inhibitor of Decaprenylphosphoryl-β-D-ribose-2′-epimerase (DprE1), holds potential for the study of tuberculosis.

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

LK-60 is a potent inhibitor of DprE1. It effectively suppresses the proliferation of Mycobacterium tuberculosis. Additionally, LK-60 demonstrates good safety profiles for gut microbiota and human cells.

Cmpd 339509 is a DprE1 inhibitor. DprE1 is an epimerase required for cell wall biosynthesis.

OPC-167832 is a highly potent and orally bioavailable dprE1 inhibitor with an IC₅₀ of 0.258 μM. It exhibits anti-mycobacterial activity against Mycobacterium tuberculosis and can be used in tuberculosis-related research.

Antitubercular agent-32 is a Benzothiazinone derivative that inhibits Mycobacterium tuberculosis and exhibits good metabolic stability and water solubility. Antitubercular agent-32 can act on decaprenylphosphoryl-β-D-ribose 2'-oxidase (DprE1, IC50: 3.9 μM) and exhibits antitubercular effects.

Antitubercular agent-31 is an antitubercular agent that inhibits M. tuberculosisH37Rv (MIC: 0.03 μM) and also inhibits DprE1 (IC50: 1.1 μM).

Antimycobacterial agent-6 (compound 25) effectively inhibits Mycobacterium tuberculosis, including wild-type and fluoroquinolone-resistant strains, by targeting the Mtb DprE1-C387S mutant, with minimal inhibitory concentrations (MIC90) of 0.9 μM for H37Rv and MoxR strains, and 0.5 μM for the DprE1-P116S strain [1].