anti-tuberculosis

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

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

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

DprE1-IN-2 is an effective DprE1 inhibitor.

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-10 (Compound 9) demonstrates antibacterial activity against Mycobacterium tuberculosis with a MIC of 0.3 μM. It exerts its antimicrobial effects by targeting the bacterial 50S ribosomal subunit, thereby inhibiting protein synthesis. Additionally, Antituberculosis agent-10 is active when administered orally.

Antituberculosis agent-15 (Compound 18c) is a selective antimycobacterial agent with a minimum inhibitory concentration (MIC) of 0.45 μM against Mycobacterium tuberculosis H37Rv (ATCC 27294) and 0.28 μM against its wild-type strain H37Rv-LP (ATCC 25618). It exhibits potent intracellular inhibitory activity in macrophage infection models, with an IC50 of 0.16 μM. Antituberculosis agent-15 is applicable for tuberculosis research.

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.

DuP-721 is a broad-spectrum, orally active antibacterial agent that inhibits a variety of clinically susceptible and resistant bacteria, particularly [M. tuberculosis].

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.

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

LeuRS-IN-1 is an orally active and potent Mycobacterium tuberculosis leucyl-tRNA synthetase inhibitor with anti-leukemic and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in leukemia research.

IMPDH2-IN-2 is a potent inhibitor of inosine 5'-monophosphate dehydrogenase (IMPDH) (Ki,app: 14 μM) and a potential anti-tuberculosis agent, exhibiting moderate antibacterial effects with MIC values of 6.3 and 11 μM in minimal GAST/Fe and rich 7H9/ADC/Tween media, respectively.

LeuRS-IN-1 hydrochloride is an orally active and highly potent inhibitor of Mycobacterium tuberculosis leucyl-tRNA synthetase with anti-leukemic activity and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in the study of leukemia.

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

1-Hydroxy-2-butanone, a natural product extractable from bamboo juice and tomato leaves, exhibits anti-tuberculosis activity.