Antituberculosis agent-5 is a small molecule used for high-throughput assays.

Antituberculosis agent-7, an oxetanyl-quinoline derivative, exhibits potent antibacterial activity against P. mirabilis, with a minimum inhibitory concentration (MIC) of 31.25 μM, and antifungal efficacy against A. niger, with a MIC of 62.5 μM. Furthermore, it demonstrates remarkable antimycobacterial activity, achieving a MIC of 3.41 μM against M. tuberculosis H37Rv [1].

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

Antituberculosis agent-3 is an antituberculosis agent with antimycobacterial activity and inhibited the growth of Mycobacterium tuberculosis strain H37Rv with a MIC value of 12.5 μg/mL.

Antituberculosis agent-9 (Compound 5a), an orally administered compound, demonstrates potent antitubercular activity, exhibiting a minimum inhibitory concentration (MIC) of 0.5 μg/mL against H37Ra [1].

Antituberculosis agent-8 is an antitubercular compound effective against M. tuberculosis H37Rv, demonstrating a minimum inhibitory concentration (MIC) of 3.53 μM (1.6 μg/mL). Additionally, it exhibits potent antifungal properties against A. niger, with an MIC of 62.50 μM.

Antituberculosis agent-6 is a potent antimycobacterial and antifungal compound with significant activity against M. tuberculosis (MIC of 3.49 μM) and A. niger (MIC of 62.50 μM), respectively. It also demonstrates high gastrointestinal (GI) absorption.

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].

D-Cycloserine (RO-1-9213) is a broad spectrum antibiotic used as a second line agent for treatment of drug resistant tuberculosis, always in combination with other antituberculosis agents.

NITD-916 is an orally active and highly lipophilic inhibitor of Mycobacterium enoyl reductase InhA with an IC50 of 570 nM.NITD-916 is a potent 4-hydroxy-2-pyridone derivative that forms a ternary complex with InhA and NADH, preventing access to the fatty acyl substrate-binding pocket.NITD-916 exhibits antituberculosis activity.

Chrysomycin A is an antibiotic that can be derived from Streptomyces. Chrysomycin A, Chrysomycin A inhibits cancer cell proliferation, migration, and invasion through the Akt/GSK-3β/β-catenin signaling pathway. Exhibits antitumor antituberculosis and MRSA activity.

DprE1-IN-2 is an effective DprE1 inhibitor.

Carbazomycin A is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities.1,2It is active againstS. aureus,T. asteroides, andT. mentagrophytes(MIC = 12.5 μg/ml for all), as well as the plant pathogenic fungusP. oryzae(MIC = 25 μg/ml). Carbazomycin A is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 26.2, 30.1, 18.4, and 32.6 μg/ml, respectively).2 1.Sakano, K.-I., Ishimaru, K., and Nakamura, S.New antibiotics, carbazomycins A and B. I. Fermentation, extraction, purification and physico-chemical and biological propertiesJ Antibiot. (Tokyo)33(7)683-689(1980) 2.Intaraudom, C., Rachtawee, P., Suvannakad, R., et al.Antimalarial and antituberculosis substances from Streptomyces sp. BCC26924Tetrahedron67(39)7593-7597(2011)

Carbazomycin D is a bacterial metabolite that has been found inStreptomycesand has diverse biological activities.1,2It is active against the fungiT. asteroidesandT. mentagrophytes(MIC = 100 μg/ml for both) and the bacteriumM. tuberculosis(IC50= 25 μg/ml). Carbazomycin D is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 21.3, 33.2, 12.9, and 34.3 μg/ml, respectively).2 1.Naid, T., Kitahara, T., Kaneda, M., et al.Carbazomycins C, D, E and F, minor components of the carbazomycin complexJ. Antibiot. (Tokyo)40(2)157-164(1987) 2.Intaraudom, C., Rachtawee, P., Suvannakad, R., et al.Antimalarial and antituberculosis substances from Streptomyces sp. BCC26924Tetrahedron67(39)7593-7597(2011)

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

DHFR-IN-10 (compound 4c) is a potent inhibitor of dihydrofolate reductase (DHFR), displaying an inhibition concentration half-maximum (IC50) of 4.21 μM against Mycobacterium tuberculosis DHFR enzyme and demonstrates strong antituberculosis efficacy [1].

Cefsulodin sodium (Sulcephalosporin) hydrate is a β lactam antibiotic.

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.

Q151 is an IMPDH inhibitor. It also is a potential antituberculosis agent.

Sativan possesses a broad spectrum of antimicrobial activity against bacteria and phytopathogenic fungi, it exhibits antituberculosis activity against Mycobacterium tuberculosis H37Rv, with the MIC value of 50 ug/mL.

Imidazoleacetic acid hydrochloride (I4AA) is an imidazole derivative with potential antituberculosis properties. It also used in the preparation of acyl guanidine inhibitors of β-secretase.

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

Antitubercular Agent-38, a derivative of Benzothiazinones (BTZs), demonstrates potent antituberculosis activity while maintaining low cardiac toxicity and minimal cell cytotoxicity [1]. This orally active compound is a promising therapeutic in the treatment of tuberculosis.

Danshenxinkun D has antituberculosis H_(37)Rv activity in vitro.

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.

MptpB-IN-2 (compound 20), a selective inhibitor for mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB), exhibits half maximal inhibitory concentrations (IC50) of 0.64 μM for MptpB, 4.06 μM for MptpA, and 4.14 μM for PTP1B. Despite its inhibition potency, MptpB-IN-2 demonstrates limited antituberculosis efficacy, with a minimum inhibitory concentration (MIC) of 64.9 μM against Mtb H37Rv [1].

Golotimod hydrochloride (SCV 07 hydrochloride) is an immunomodulating peptide with antimicrobial properties. It enhances antituberculosis therapy effectiveness, promotes thymic and splenic cell proliferation, and boosts macrophage functionality. Furthermore, it inhibits STAT3 signaling, thereby modifying the duration and intensity of oral mucositis in animal models subjected to radiation or a combination of radiation and Cisplatin. Additionally, Golotimod hydrochloride has shown potential as a treatment for recurrent genital herpes simplex virus type 2 (HSV-2) [1] [2] [3].