antituberculosis

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

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

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

Antituberculosis agent-12 (compound 3408) is a narrow-spectrum prodrug of a phosphate, designed to inhibit resistant tuberculosis infections.

Antituberculosis agent-13 (Compound 11) demonstrates antituberculosis activity, effectively inhibiting both wild-type and mutant strains of Mycobacterium tuberculosis, with an IC50 range of 4-62.5 nM. Additionally, Antituberculosis agent-13 exhibits anti-leukemia properties, inhibiting MOLM-13 with an IC50 of 3.8 μM.

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].

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].

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

Methyl α-D-mannopyranoside (Methyl α-D-mannopyranoside) can be used as an intermediate for chemical sythesis and can target macrophages in anti-tuberculosis inhalation therapy[1].

Isosteviol ((-)-Isosteviol), a common natural sweetener, belongs to tetracyclic diterpene glycosides. The pharmacology researches have suggested that stevioside and its hydrolysis products, steviol, isosteviol and steviolbioside, have many biological activities, such as reducing blood glucose, lowering blood pressure, anti-inflammation, anti-tumor, anti-diarrhea, antibacterium, immunoregulation, etc.

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.

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.

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.

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.

RCB18350 is an antituberculosis agent and an isoxazole derivative. It demonstrates bacteriostatic properties by inhibiting the growth of Mycobacterium tuberculosis, with a minimum inhibitory concentration (MIC) of 1.25 μg/mL. RCB18350 is effective against multi-drug resistant Mycobacterium tuberculosis (MDR-TB) clinical isolates, Mycobacterium bovis BCG, and Mycobacterium avium, all of which are slow-growing mycobacteria.

Carbonic anhydrase inhibitor31 is an mtCA2 inhibitor (Ki: 5.2 nM) that can be used in antituberculosis research.

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

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

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.

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)