Tuberculosis inhibitor 5

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

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.

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.

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

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

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

Antimycobacterial agent-10 (compound 5) is an inhibitor of DNA gyrase with an IC50 of 96 nM against Mycobacterium tuberculosis gyrase, demonstrating antibacterial properties.

Topoisomerase inhibitor 5 (compound 158) is an inhibitor of bacterial topoisomerase, with a minimum inhibitory concentration of 0.125 μg mL, and exhibits anti-tuberculosis activity.

DXR-IN-4 (Compound 12a) is an inhibitor of 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR). It effectively inhibits DXR in Plasmodium falciparum, Escherichia coli, and Mycobacterium tuberculosis, with IC50 values for PfDXR, EcDXR, and MtDXR at 18, 4.9, and 89 nM, respectively. Additionally, DXR-IN-4 demonstrates antimalarial activity against Plasmodium falciparum strains 3D7 and Dd2, with IC50 values of 11 μM and 12 μM.

MtTMPK-IN-5 (compound 17) is a highly effective inhibitor of M. tuberculosis thymidylate kinase (Mtb TMPK), demonstrating remarkable enzyme inhibitory activity with an IC50 of 34 μM. Additionally, MtTMPK-IN-5 exhibits notable activity against M. tuberculosis, with an MIC of 12.5 μM. Given its potent properties, MtTMPK-IN-5 serves as a valuable tool 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].

Mt KARI-IN-5 (compound 6c) was a potent inhibitor of Mycobacterium tuberculosis ketohydrin reductase I (MtbKARI) (Ki: 4.72 μM), exhibited inhibition of MtbH37Rv activity with a MIC value of 1.56 μM, showed low cytotoxicity, and had an IC50 value for HEK greater than 64 μg mL.

MtTMPK-IN-2 (compound 15), a potent inhibitor of Mycobacterium tuberculosis thymidylate kinase (Mt TMPK), demonstrates an IC50 value of 1.1 μM. This compound effectively inhibits Mtb H37Rv with a minimum inhibitory concentration (MIC) of 12.5 μM and exhibits cytotoxicity in MRC-5 human fibroblast cells with an EC50 of 6.1 μM. MtTMPK-IN-2 is valuable for tuberculosis research [1].

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].

C82 acts as an inhibitor of Mycobacterium tuberculosis (Mtb) cyclic dinucleotide phosphodiesterase (CdnP), with an IC50 value of 17.5 µM. This particular enzyme is responsible for breaking down cyclic di-AMP (c-di-AMP) into adenosine 5'-monophosphate (AMP). Notably, C82 demonstrates selectivity for Mtb CdnP over other bacterial cyclic dinucleotide phosphodiesterases (CDN PDEs) such as Yybt, RocR, and Group B Streptococcus (GBS) CdnP, as well as the mammalian CDN PDE ENPP1, and the viral CDN PDE poxin, showing effectiveness at a concentration of 200 µM.

5'-Azido-5'-deoxythymidine is a nucleoside analog with potential anti-tuberculosis activity as an inhibitor of Mycobacterium tuberculosis monophosphate kinase (TMPKmt), an enzyme essential for DNA replication in Mycobacterium tuberculosis. 5'-Azido-5'-deoxythymidine contains an azide group in its molecular structure, which enhances its ability to inhibit reverse transcriptase, and is commonly used in the study of nucleoside metabolic pathways and related disease mechanisms.