antitubercular

Pyrazinamide (Pyrazinecarboxamide), an antimycobacterial, is utilized therapeutically as an antitubercular agent, which is a synthetic pyrazinoic acid amide derivative.

Antitubercular agent-30 has antitubercular activity.

Antitubercular agent-47 (compound 5C) exhibits potent activity against tuberculosis and is effective against DS MDR XDR clinical isolates.

Antitubercular agent-10 exhibits potent antitubercular activity with a MIC value of 30 nM.

Antitubercular agent-9 exhibits potent activity against tuberculosis, demonstrating a minimum inhibitory concentration (MIC) range of 1.03-2.32 μM.

Antitubercular agent-41 is a antibacterial agent.

Antitubercular agent-28 (compound 2) exhibits antimycobacterial activity against resistant isolates of Mycobacterium tuberculosis H37Rv with an MIC of 4.5 μM, an IC50 of 1.5 μM, and an IC90 of 2.5 μM. It demonstrates effective intracellular antimycobacterial activity with low cytotoxicity [1].

Antitubercular agent-11 (Compound 1e) contains a bulkier electron-donating group (Bu-t) and exhibits the best MIC value of 0.060 μg mL [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-14 (Compound 1) exhibits antitubercular activity with an MIC value of 0.3 μg mL against M. tuberculosis [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-27 (compound 1) exhibits potent antitubercular properties with an IC50 of 3.2 μM, an MIC of 7.8 μM, and an IC90 of 7.0 μM, effectively targeting resistant Mycobacterium tuberculosis H37Rv isolates and displaying significant intracellular antimycobacterial activity with low cytotoxicity [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].

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-13 (Compound 3d) is an antitubercular compound with MIC values of 0.007 μg mL against MTB H37Rv and 1.851 μg mL against MDR-MTB 16833, respectively, and exhibits metabolic instability [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].

Antitubercular agent-12 (Compound 2c) is a highly effective antitubercular agent with a MIC (Minimum Inhibitory Concentration) value of 1.439 μg mL and significantly reduced cytotoxicity, evidenced by a CC50 (50% Cytotoxic Concentration) value of 57.34 μg mL [1].

Antitubercular agent-25 (Compound 28) is an anti-tubercular agent with an extracellular IC50 of 0.42 μM and an intracellular IC50 of 0.20 μM against M. tuberculosis H37Rv, and it demonstrates good metabolic stability.

Antitubercular agent-29 (compound 6xa) is a potent Mycobacterium tuberculosis (Mtb) inhibitor, effective against drug-resistant (DR) and drug-susceptible (DS) strains with a minimum inhibitory concentration (MIC) of 0.03 μg mL for DS-Mtb and 0.03-0.06 μg mL for DR-Mtb strains, and demonstrates favorable selectivity (SI>40) against Vero cells.

Antitubercular agent-26 (Compound 32) is an orally active agent targeting M. tuberculosis H37Rv cells with an IC50 of 0.50 μM extracellularly and 0.51 μM intracellularly. It exhibits good metabolic stability, a low risk of cardiotoxicity, and no genotoxicity.

Antitubercular agent-32 is a Benzothiazinone derivative that inhibits Mycobacterium tuberculosis and exhibits good metabolic stability and water solubility. Antitubercular agent-32 can act on decaprenylphosphoryl-β-D-ribose 2'-oxidase (DprE1, IC50: 3.9 μM) and exhibits antitubercular effects.

Antitubercular agent-31 is an antitubercular agent that inhibits M. tuberculosisH37Rv (MIC: 0.03 μM) and also inhibits DprE1 (IC50: 1.1 μM).

Antitubercular agent-23 is an effective anti-Candida and anti-tuberculosis agent against Candida albicans MTCC 3017 (MIC: 1.1 μg ml) and M. tuberculosis (H37Rv) (MIC: 1 μg ml).