h37rv

Anti-TB agent 1 is a potent and orally active anti-tuberculosis compound (MICs: < 2 nM against the Mtb strains H37Rv, rRMP, and rINH).

Urease Inhibitor 07 is an isosubstituted metalloproteinase inhibitor with potential activity against Mycobacterium tuberculosis strain H37Rv.

Thiacetazone (Diazam) is a thiosemicarbazone that thioacetazone treatment of pulmonary tuberculosis

sCNH240 (2-Fluoro-N-[3-(3-thienyl)-5-isoxazolyl]benzenesulfonamide) is a potential and selective Rv1625c Cya activator with good cell permeability and oral activity, IC90=1.24 μM in cholesterol-supplemented 7H12 medium against Mycobacterium tuberculosis (Mtb) H37Rv strain, and inhibition of CYP2C19, CYP2C9 and hERG channels.

TBA-354 is anti-tuberculous and active against Mycobacterium tuberculosis strain H37Rv.

BM635 is an MmpL3 inhibitor with outstanding anti-mycobacterial activity (MIC50: 0.12 μM against M. tuberculosis H37Rv).

BM635 hydrochloride is an MmpL3 inhibitor with outstanding anti-mycobacterial activity (MIC50: 0.12 μM against M. tuberculosis H37Rv).

BM635 mesylate is an MmpL3 inhibitor with outstanding anti-mycobacterial activity (MIC50: 0.12 μM against M. tuberculosis H37Rv).

MDRTB-IN-1 (5aα) is an antibiotic effective against Mycobacterium tuberculosis H37Rv, with a MIC90 of 10.5 μM.

NITD-349 is an inhibitor of MmpL3. It shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.

Mtb-IN-8 (compound 5jb) serves as an orally active inhibitor specifically targeting Mycobacterium tuberculosis (Mtb). It exhibits a minimum inhibitory concentration (MIC) of 0.03 μg mL against H37Rv strains and ranges from 0.125 to 0.06 μg mL against multi-drug resistant Mtb (MDR-Mtb).

VEGFR-2 InhA-IN-1, a dual inhibitor based on pyrazole, targets InhA and VEGFR, exhibiting both anti-tuberculosis and anti-angiogenic properties. It demonstrates effective antibacterial activity against the Mycobacterium tuberculosis H37Rv strain (MIC = 6.25 μg mL) and significantly suppresses VEGFR-2 activity (IC 50 = 15.27 nM).

ATP synthase inhibitor3 (compound PT6) is an orally active inhibitor targeting the F-ATP synthase of Mycobacterium tuberculosis (IC50=0.788 μM). It effectively inhibits the growth of the Mycobacterium tuberculosis H37Rv strain (ATCC-27294) in vitro, depleting intracellular ATP levels at an IC50 of 30 μM.

InhA-IN-8 (compound 6c) serves as an orally effective inhibitor of the Mycobacterium tuberculosis enzyme InhA (enoyl-ACP reductase). This compound demonstrates robust inhibitory activity against Mtb H37Rv, with a minimum inhibitory concentration (MIC) ranging from 0.5 to 1 μg mL. Additionally, InhA-IN-8 is utilized in studies involving acute tuberculosis models in mice.

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).

HT1171 is a potent and selective inhibitor of the Mycobacterium tuberculosis proteasome. It exhibits strong antitubercular activity against Mycobacterium tuberculosis H37Rv, with a MIC90 of 2 μg mL and MIC of 4 μg mL. At a concentration of 100 μM, HT1171 shows an inhibition rate of 53.8% against normal human liver cells (L02). HT1171 is applicable in antituberculosis drug research.

Pks13-IN-1 (Compound 44) is an orally active inhibitor of Mycobacterium tuberculosis polyketide synthase 13 (Pks13). It inhibits the M. tuberculosis H37Rv strain with a minimum inhibitory concentration (MIC) of 0.07 μM. In mouse models, Pks13-IN-1 demonstrates antibacterial activity.

Pks13-IN-2 (Compound 43) is an orally active inhibitor of Pks13. It exhibits inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 0.8-1.8 μM. Pks13-IN-2 demonstrates good metabolic stability in mouse liver microsomes and hepatocytes, making it suitable for tuberculosis research.

SB-790594-A is a non-cytotoxic Mycobacterium tuberculosis H37Rv inhibitor.

GSK1829820A is a Mycobacterium tuberculosis H37Rv non-cytotoxic inhibitor.

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

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg/ml) and Kurono (MIC: 0.0005 μg/ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg/ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg/ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg/ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg/kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1/2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg/kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg/kg to 2.5 mg/kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg/kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.

Tuberculosis inhibitor 3 (compound 2i) is a highly potent and orally bioavailable anti-tuberculosis drug with in vitro antidrug activity of MIC < 0.016 μg mL against both drug-sensitive and drug-resistant Mycobacterium tuberculosis, H37RV & MDR-TB.

Polyketide synthase 13-IN-3 (compound 41) is a potent inhibitor of polyketide synthase 13, with a minimum inhibitory concentration (MIC) range of 0.0625-0.125 μg mL against the M. tuberculosis strain H37Rv.