tuberculosis inhibitor 3

Tuberculosis inhibitor 3 (compound 2i) is a highly potent and orally bioavailable anti-tuberculosis drug with in vitro antidrug activity of MIC < 0.016 μg mL against both drug-sensitive and drug-resistant Mycobacterium tuberculosis, H37RV & MDR-TB.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

JFD01307SC ([(1,1-DIOXIDOTETRAHYDROTHIEN-3-YL)AMINO]) is a glutamine synthetase inhibitor. It is anti-tuberculosis agent and acts as a mimic of L-Glutamate and thus target enzymes involved in glutamine biosynthesis.

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

Enzyme-IN-3 disodium (compound 7) is a selective inhibitor of Mycobacterium tuberculosis shikimate kinase with an IC50 of 1.6 μM. Additionally, Enzyme-IN-3 disodium exhibits antibacterial properties.

Polyketide synthase 13-IN-3 (compound 41) is a potent inhibitor of polyketide synthase 13, with a minimum inhibitory concentration (MIC) range of 0.0625-0.125 μg mL against the M. tuberculosis strain H37Rv.

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.

MmpL3-IN-1, also known as compound 32, is a highly effective inhibitor of Mycobacterial membrane protein large 3 (MmpL3). With an anti-tuberculosis activity exhibiting a minimum inhibitory concentration (MIC) of less than 0.016 μg mL in M. tuberculosis, MmpL3-IN-1 is a valuable compound for research on drug-resistant tuberculosis [1].

PptT-IN-3 (compound 5p) is a powerful inhibitor (IC50 = 3.5 μM) of phosphopantetheinyl phosphoryl transferase (PptT), an indispensable enzyme involved in the synthesis of cellular lipids and virulence factors in Mycobacterium tuberculosis. This compound holds promise for tuberculosis research [1].

MtTMPK-IN-1 (compound 3) is a highly effective inhibitor of Mycobacterium tuberculosis thymidylate kinase (Mt TMPK), with an IC50 value of 2.5 μM. It shows moderate to weak activity against Mtb H37Rv and low cytotoxicity in human fibroblast cells MRC-5, making it a valuable tool for tuberculosis research [1].

DNA Gyrase-IN-3 (Compound 28) is an inhibitor of bacterial DNA gyrase B with an IC50 of 5.41-15.64 μM for inhibiting Escherichia coli DNA rotatase. It exhibits both anti-tuberculosis and antibacterial activity.

UGM-IN-3 (compound 10a) is an inhibitor of UDP-galactopyranose mutase (UGM) with a Kd of 66 μM and inhibits the growth of Mycobacterium tuberculosis (MIC= 6.2 μg mL).

MtTMPK-IN-3 (compound 25) is a potent inhibitor of Mycobacterium tuberculosis thymidylate kinase (MtTMPK) with an IC50 value of 0.12 μM. It also exhibits inhibitory activity against Mtb H37Rv with a MIC of 12.5 μM and shows cytotoxicity in MRC-5 human fibroblast cells (EC50 = 12.5 μM). This compound is useful for tuberculosis research [1].

Mtb-cyt-bd oxidase-IN-3, an inhibitor of Mycobacterium tuberculosis cytochrome bd oxidase (Mtb cyt-bd oxidase), exhibits an IC50 value of 0.36 μM and demonstrates an ability to inhibit the growth of Mycobacterium tuberculosis with an MIC of 32 μM. This compound is utilized in tuberculosis research.

Mtb-IN-3 (compound 10c), a selective and potent Mycobacterium tuberculosis (Mtb) inhibitor, exhibits strong antimycobacterial activity in vitro without inducing cytotoxic effects and inhibits colony formation in the spleen in murine tuberculosis models [1].

MmpL3-IN-3 (Compound 12), an MmpL3 inhibitor, exhibits potent anti-tuberculosis activity with a minimum inhibitory concentration (MIC) of 0.1 μM against H37Rv and demonstrates good metabolic stability in mouse liver microsomes. This compound is valuable for anti-tubercular research [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 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].

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 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].

Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.