tuberculosis

Tuberculosis inhibitor 5 (Compound 11i) is a potent antimycobacterial biphenyl analogue and anti-tuberculosis agent with no apparent cytotoxicity.

Tuberculosis inhibitor 1 is a potent, non-cytotoxic inhibitor of Trypanosoma brucei growth [EC50: 5 nM].

Tuberculosis inhibitor 8 (compound 3b), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against both Mycobacterium tuberculosis and Mycobacterium marinum with an MIC 90 of 0.69 μM [1].

Tuberculosis inhibitor 4 (compound 16) is a spirothiazolidinone derived from mandelic acid, exhibiting potent antimycobacterial activity by inhibiting 98% of Mycobacterium tuberculosis strain H37Rv at concentrations below 6 μg mL.

Tuberculosis Inhibitor 12, an oxadiazole derivative, effectively inhibits Mycobacterium tuberculosis, demonstrating inhibition rates of 82% and 78% at a concentration of 20 μM on 7H9-Tw-OADC media, respectively [1].

Tuberculosis Inhibitor 10 moderately inhibits the enzyme MSMEG_6649 and potentiates the antimycobacterial activity of PAS [1].

Tuberculosis inhibitor 9 (compound 3d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and Mycobacterium marinum, with an MIC 90 of 0.64 μM for both organisms [1].

Tuberculosis inhibitor 6 (compound 2c), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, is highly active against Mycobacterium tuberculosis (MIC 90 of ≤1.66 μM) and Mycobacterium marinum (MIC 90 of 2.65 μM) [1].

Tuberculosis inhibitor 3 (compound 2i) exhibits potent anti-TB properties (MIC < 0.016 μg mL) against both drug-sensitive and resistant MTB strains, with acceptable pharmacokinetic profiles and oral bioavailability[1].

Mycobacterium Tuberculosis-IN-2 (Compound 29) acts as a potent bacterial inhibitor specifically targeting Mycobacterium Tuberculosis, making it useful for tuberculosis research (MIC = 0.07-0.16 μM) [1].

Tuberculosis inhibitor 7 (compound 2d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and Mycobacterium marinum, with both displaying a MIC 90 of 0.63 μM [1].

Mycobacterium Tuberculosis-IN-5 (Compound 11) is the hydrochloride salt form of 5-Fluoroindole. It acts as an antimicrobial agent effective against Mycobacterium tuberculosis with a minimum inhibitory concentration (MIC) of 29.1 μM. This compound demonstrates metabolic stability in rat liver microsomes and exhibits antitubercular activity in mice.

Compound 14, also known as Tuberculosis Inhibitor 11, enhances the antimycobacterial efficacy of antitubercular agent [1].

timcodar is a non-FKBP12 binding macrolide derivative that is an efflux pump inhibitor with antimicrobial activity, inhibition of lipid accumulation, inhibition of Mycobacterium tuberculosis, and can be used in the study of obesity. timcodar is a non-FKBP12 binding macrolide derivative with antimicrobial activity.

Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor that reduces the production of pro-inflammatory mediators and cytokines. Dovramilast is used in the study of Mycobacterium tuberculosis infections and lupus erythematosus.

16α-Bromoepiandrosterone (BEA) is a water-soluble synthetic sterol related to DHEA and is used in studies of type II diabetes and non-diabetic 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).

GSK572A is a novel and potent potent inhibitor of EchA6, which can be used to treat tuberculosis.

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 is a highly potent and orally active inhibitor of the leucyl-tRNA synthetase enzyme derived from Mycobacterium tuberculosis (M.tb LeuRS). It exhibits significant inhibitory activity against M.tb LeuRS with IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively. Additionally, LeuRS-IN-1 effectively inhibits human cytoplasmic LeuRS with an IC 50 value of 38.8 μM and suppresses protein synthesis in HepG2 cells with an EC 50 value of 19.6 μM.

Thiacetazone (Diazam) is a thiosemicarbazone that thioacetazone treatment of pulmonary tuberculosis

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

Rifampicin (Rifamycin AMP) is a broad-spectrum antibiotic. Rifampicin has a strong antibacterial effect against Mycobacterium tuberculosis and is also effective against gram-positive and gram-negative bacteria and viruses.

Cloxiquine (Dermofongin) is a monohalogenated 8-hydroxyquinoline with activity against bacteria, fungi, and protozoa.

Bedaquiline fumarate (TMC207), a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections. It blocks the proton pump for ATP synthase of mycobacteria. It is the first member of a new class of drugs called diarylquinolines.

Faropenem sodium is an orally bioavailable penem antibiotic effective in treating Mycobacterium tuberculosis, as well as tuberculosis and community-acquired pneumonia.

Rifamycin S is a potent DNA-dependent RNA polymerase inhibitor,is a quinone and an antibiotic agnet against Gram-positive bacteria

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.

Kanamycin sulfate (Kanamycin monosulfate) is an aminoglycoside antibiotic that interferes with protein synthesis by binding to the 70S ribosomal subunit of bacteria. Kanamycin sulfate exhibits antimicrobial activity against both Gram-positive and Gram-negative bacteria, as well as mycoplasmas.

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.

Mtb-IN-2 is a small molecule compound of Mycobacterium tuberculosis (Mtb) with antimicrobial activity and low toxicity that interferes with methionine metabolism processes and can be used to study tuberculosis.

Dihydrostreptomycin sulfate (Dihydrostreptomycin sesquisulfate) inhibits protein synthesis by binding to the 30S ribosomal subunit. Dihydrostreptomycin Sulfate is a semi-synthetic aminoglycoside antibiotic with bactericidal properties. This antibiotic is active against most gram-positive and gram-negative organisms and is used in the treatment of tuberculosis and tularemia.

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].

Methyl quinoline-2-carboxylate (Methyl 2-quinolinecarboxylate) inhibits the binding of Mycobacterium tuberculosis.

Urease Inhibitor 07 is an isosubstituted metalloproteinase inhibitor with potential activity against Mycobacterium tuberculosis strain H37Rv.

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

Sodium 4-aminosalicylate dihydrate (4-Amino-salicylic acid sodium salt) is the sodium salt form of aminosalicylic acid, an analog of para-aminobenzoic acid (PABA) with antitubercular activity. Sodium 4-aminosalicylate dihydrate exerts its bacteriostatic activity against Mycobacterium tuberculosis by competing with PABA for enzymes involved in folate synthesis, thereby suppressing growth and reproduction of M. tuberculosis, eventually leading to cell death.

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

7,3′,4′-Tri-O-methyleriodictyol (7,3;,4;-Tri-O-methyleriodictyol) is an isolate from the methanolic extract of Pogostemon cablin with antimicrobial, antioxidant, antitumor, and antiprotozoal activities, and it inhibits Mycobacterium tuberculosis infection as well as SOS-inducing activity.

Linaroside exhibited 30% inhibition for antimycobacterial activity against Mycobacterium tuberculosis, strain H(37)Rv at 6.25 microg mL(-1) concentration.

InhA-IN-3 (TU13) is a potent inhibitor of Mycobacterium tuberculosis InhA (enoyl ACP reductase) with potential anticancer and antiproliferative activities for the study of Mycobacterium tuberculosis infections.

InhA-IN-2 directly inhibits InhA and does not require activation by the catalase peroxidase KatG.

ND-011992 is a reversible and selective quinazoline inhibitor targeting quinone reductases and quinol oxidases.ND-011992 inhibits E. coli BL21*Δcyo respiratory complex I. ND-011992 inhibits bo3 oxidase, bd-I oxidases and bd-II oxidases, ND-011992 inhibits E. coli BL21*Δcyo respiratory complex I, bo3 oxidase, bd-I oxidases, and bd-II oxidases with IC50s of 0.12, 2.47, 0.63, and 1.3 μM, respectively.ND-011992 can be used in the study of tuberculosis.

VCC234718 is a molecule with growth inhibitory activity against Mycobacterium tuberculosis (Mtb).

Piperlotine A is an alkaloid that can be extracted from Piperonyssinus rolfsii and has antiplatelet aggregation activity.Piperlotine A showed inhibition of Mycobacterium tuberculosis in an in vitro assay with a MIC value of 50 ug/mL.Piperlotine A is an alkaloid that can be extracted from Piperonyssinus rolfsii and has antiplatelet aggregation activity.

InhA-IN-4 (TU14) is a potent inhibitor of Mycobacterium tuberculosis InhA (enoyl ACP reductase), with potential anticancer and antiproliferative activities for studying Mycobacterium tuberculosis infections.

GSK2556286 (GSK286) is an orally active inhibitor of Mycobacterium tuberculosis (M. tuberculosis), effective against multidrug-resistant (MDR), extensively drug-resistant (XDR), and drug-sensitive (DS) strains. It inhibits the growth of human macrophages with an IC50 value of 0.07 μM.

AU1235 is a Mycobacterium tuberculosis inhibitor.