anti-tuberculosis

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].

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

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-17 (compound 21) is a potent and selective antituberculosis agent. It demonstrates excellent antituberculosis activity against Mycobacterium tuberculosis H37Rv, multidrug-resistant (MDR) strains, and extensively drug-resistant (XDR) strains, with MIC values ranging from 0.2 to 0.78 μM. Its selectivity is higher for Mycobacterium tuberculosis than for certain non-tuberculous mycobacteria and bacteria. Antituberculosis agent-17 is applicable in 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].

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

SQ109 (NSC 722041) is an ethambutol (EMB) derivative and a specific inhibitor of MmpL3, exhibiting potent anti-Mycobacterium tuberculosis activity. SQ109 effectively inhibits the adult stage of the parasite Trypanosoma and kills cells, with an IC50 of 50 ± 8 nM. SQ109 can be used in tuberculosis and antiparasitic research.

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.

NITD-916, a 4-hydroxy-2-pyridone derivative, is a mycobacterial enoyl reductase InhA inhibitor (IC50=570 nM) with oral activity and high lipophilicity. Capable of forming a ternary complex with InhA and NADH, blocking fatty acyl substrate binding and inhibiting mycolic acid synthesis, thereby exerting potent anti-tuberculosis effects.

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.