m. tuberculosis h37rv

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

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.

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).

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.

JNJ-2901 is an inhibitor of M. tuberculosis cytochrome bc1:aa3. It effectively reduces bacterial load in acute and chronic mouse infection models of M. tuberculosis H37Rv-ΔcydAB. JNJ-2901 is useful for tuberculosis (TB) research.

Antitubercular agent-42(19) is a selective inhibitor of fatty acyl-AMP ligase (FAAL), demonstrating a MIC90 of 1.4 µg/mL against M. tuberculosis H37Rv, and possesses antitubercular activity.

Mtb-IN-7 (compound R7) is a MAO-A/MAO-B inhibitor with an IC50 greater than 40 μM. It exhibits antibacterial activity against Mycobacterium tuberculosis H37Rv, with a MIC of 2.01 μM.

Antibacterial agent 228 (Compound 8) inhibits mycobacterial ribosomes with an IC50 of 2.31 μM against Mycobacterium smegmatis. It demonstrates antibacterial activity with MIC values of 2 and 0.25 μg/mL against both wild-type and Δ1258c mutant strains of M. tuberculosis H37Rv, 8 μg/mL against wild-type and Δ2780c mutant strains of M. abscessus ATCC 19977, and 8 μg/mL against M. smegmatis.

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.

GSK2200150A is an anti-tuberculosis (TB) agent identified by high-throughput screening (HTS) campaign.

Steviolbioside (CCRIS-6025) is a natural sweetener, it presents notable inhibition on human hepatocarcinoma cell Hep3B, human breast cancer cell MDA-MB-231 and human pancreatic cancer cell BxPC-3, thus, steviolbioside(CCRIS-6025) could be a potential remedy for human breast cancer. Steviolbioside exhibits moderate antituberculosis activity against M. tuberculosis strain H37RV in vitro.

Q203 (Telacebec) is a novel potent anti-tuberculosis agent targeting cytochrome b subunit qcrB and inhibits M. tuberculosis H37Rv (MIC50: 2.7 nM).

TBAJ-587 is a potent anti-tuberculosis agent. TBAJ-587 inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 µg/mL in MABA and LORA assay, respectively. BAJ-587 has more potent activity against M. tuberculosis and better efficacy in animal mode

Antituberculosis agent-2 (Compound 8d) is effective against both multidrug-resistant and drug-sensitive tuberculosis, exhibiting favorable microsomal stability in mouse and human, low cytotoxicity, and acceptable oral bioavailability. The MIC values against M. tuberculosis H 37 R v, 13946, and 14862 are 0.454, 1.757, and 1.644 μg/mL, respectively [1].

Antitubercular agent-15 (Compound 5n) is an antitubercular agent with low cytotoxicity against pulmonary fibroblasts and macrophages. The MIC90 values against M. tuberculosis H37Rv, CF16, CF61, CF76, CF152, and CF161 are 0.73, 7.69, 9.38, 18.80, 7.53, and 7.31 μg/mL, respectively [1].

Antitubercular agent-21 (Compound 15) is an antitubercular agent with low cytotoxicity, exhibiting an MIC of 0.4 μg/mL against M. tuberculosis H37Rv. However, it shows lower activity against other microorganisms, including gram-positive bacteria, gram-negative bacteria, and fungi [1].

Antitubercular agent-17 (Compound 8a) is an efficacious antitubercular agent, demonstrating Minimum Inhibitory Concentration (MIC) values of 2 μg/ml against M. tuberculosis H37Rv, Spec. 192, and Spec. 210, and 128 μg/ml against Spec. 800. It exhibits highly selective antimycobacterial effects [1].

Antitubercular agent-18 (Compound 9a) is an antitubercular agent that exhibits highly selective antimycobacterial effects, with minimum inhibitory concentration (MIC) values of 2 μg/ml against M. tuberculosis H37Rv, Spec. 192, and Spec. 210, and 128 μg/ml against Spec. 800, demonstrating its efficacy in inhibiting the growth of these mycobacterial strains [1].

Antituberculosis Agent-1 (Compound 8a) is an effective antituberculosis agent, demonstrating a minimum inhibitory concentration (MIC) of 3.84 μg/mL against Mycobacterium tuberculosis H37Rv [1].

Antitubercular agent-16 (Compound 5q) is a potent antitubercular agent exhibiting high efficacy against various strains of M. tuberculosis, including H37Rv, CF16, CF61, CF76, CF152, and CF161, with MIC 90 values ranging from 0.40 to 23.51 μg/mL. Notably, Antitubercular agent-16 demonstrates minimal cytotoxicity towards macrophages and pulmonary fibroblasts, further highlighting its potential as a therapeutic agent [1].

Antitubercular agent-24 (Compound 1) exhibits anti-tubercular properties against M. tuberculosis H37Rv, demonstrating an extracellular IC50 of 0.83 μM and an intracellular IC50 of 0.17 μM [1].