anti-tuberculosis

Anti-TB agent 1 is a potent and orally active anti-tuberculosis compound (MICs: < 2 nM against the Mtb strains H37Rv, rRMP, and rINH).

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.

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.

Pretomanid ((S)-PA 824) , a nitroimidazole, is used as an anti-tuberculosis drug for tuberculosis with MIC less than 2.8 μM.

Delamanid (OPC-67683) is an anti-tuberculosis agent derived from the nitro-dihydro-imidazooxazole class of compounds that inhibits mycolic acid synthesis of bacterial cell wall.

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.

Bedaquiline (R207910) is an anti-tuberculosis drug which selectively inhibit the mycobacterial energy metabolism i.e. ATP synthesis and found to be effective against all states of Mycobacterium tuberculosis.

TBA-354 is anti-tuberculous and active against Mycobacterium tuberculosis strain H37Rv.

SQ609 is a potential anti-tuberculosis drug selected from a library of dipiperidine derivatives. SQ609 showed significant anti-tuberculous activity in mouse macrophages in vitro[1].

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.

NITD-349 is an inhibitor of MmpL3. It shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.

ML406 shows anti-tubercular activity via MtbbioA (DAPA synthase) enzyme inhibition(IC50 : 30 nM)

Vasicine hydrochloride (Peganine hydrochloride) (peganine hydrochloride) is an alkaloid isolated from Justicia adhatoda. It possesses an anti-tuberculosis activity.

GSK2200150A is an anti-tuberculosis (TB) agent identified by high-throughput screening (HTS) campaign.

DuP-721 is a broad-spectrum, orally active antibacterial agent that inhibits a variety of clinically susceptible and resistant bacteria, particularly [M. tuberculosis].

Mtb ATP synthase-IN-1 (compound 6ab) is a potent inhibitor of Mycobacterium tuberculosis (Mtb) ATP synthase (MIC = 0.452-0.499 μg mL) [1] that can be used in anti-mycobacterium research, showing low cytotoxicity (Vero IC 50 > 64 μg mL) and acceptable oral bioavailability with good metabolic stability.

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

Antitubercular agent-33, a 2-aminothiazole derivative, exhibits potent anti-tubercular activity against Mycobacterium tuberculosis (Mtb) [1].

WX-081 is an anti-tuberculosis agent that exhibits significant anti-mycobacterial effects against M. tuberculosisH37Rv and is able to act on drug-susceptible (DS-TB) mycobacteria (MIC: 0.083 μg/ml) and multidrug-resistant (MDR-TB) strains (MIC: 0.11 μ g/ml), showed inhibition of hERG channels (IC50: 1.89 μM).

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.

Antibacterial agent 62 is a novel redox cycle anti-tuberculosis compound exhibiting significant bactericidal activity against both growing and phenotypically resistant non-growing (nutrient deficient) bacteria.

GSK366A is an anti-TB agent against Mycobacterium bovis BCG and Mycobacterium tuberculosis, targeting MmpL3 and inhibiting EchA6.

NITD-304 is an anti-tuberculosis drug candidate for the treatment of multidrug-resistant tuberculosis (MDR-TB), showing effective activity against both MTB drug-sensitive and multidrug-resistant clinical isolates.

FadD32 inhibitor -1 has anti-tuberculosis activity and is an effective FadD32 inhibitor.

Oxyphenbutazone monohydrate, a metabolite of Phenylbutazone, exhibits anti-inflammatory properties and acts as a non-selective COX inhibitor when taken orally. It also selectively targets and kills non-replicating Mycobacterium tuberculosis [1] [2].

BM635 hydrochloride is an MmpL3 inhibitor with outstanding anti-mycobacterial activity (MIC50: 0.12 μM against M. tuberculosis H37Rv).

Porson exhibited anti-tubercular activity against Mycobacterium tuberculosis H37Rv in vitro and MICs values of 40.0 μg/mL.

Maritinone is a novel anti-tuberculosis (anti-TB) agent.

Benzothiohydrazide is an analog of isoniazid with anti-tuberculosis activity and can be used to isolate fungi and bacteria.

CRS400393 is an effective anti-mycobacterial drug , with MIC of 0.03, 2, and ≤ 0.12 µg/mL against M. abs., M. avium, M. intracellulare, and M. tuberculosis, respectively.

4-Piperidinecarboxamide is a mycobacterial aspartyl-tRNA synthetase (AspS) inhibitor and a potential anti-tuberculosis (TB) agent [1].

Anti-inflammatory agent 15 (compound 29) is a potent antimycobacterial agent used in tuberculosis (TB) research, inhibiting the growth of Mtb H37Rv and M299 with MIC50 values of 2.3 and 7.8 μM, respectively. This compound also suppresses the expression of iNOS, thereby inhibiting NO, TNF-α, and IL-1β production [1].

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).

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].

Pinafide is a rodenticide and anti-protozoal agent. Pinafide shows strong cytostatic activity against both HeLa and KB cells and is moderately toxic to both mice and rats. It has been proved active against experimental tumors and shown to be inhibitor of two DNA viruses. Pinafide blocks cell growth by inhibiting DNA and RNA synthesis. It has been shown to bind to double-helical DNA by intercalation. Pinafide inhibited the activity of M. tuberculosis NAD⁺-dependent DNA ligase A at concentrations of 50 uM. At the chemical screening was found that pinafide inhibited B-Myb transcriptional activity in luciferase assays. The cross placental-barrier studies showed that 3H-pinafide was present in the 14-day fetuses.

Ganfeborole HCl (GSK3036656 HCl) is a small molecule compound with anti-tuberculosis activity and is an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS; IC50: 0.2 μM).

Lansoprazole Sulfide D4 is a deuterium labeled Lansoprazole Sulfide. Lansoprazole Sulfide is an orally active anti-TB (Mycobacterium tuberculosis) agent with IC50 values of 0.59 μM intracellularly and 0.46 μM in broth.Lansoprazole Sulfide is an active metabolite of the proton pump inhibitor Lansoprazole.

Mycobacterial Zmp1-IN-1, a zinc metalloprotease-1 (Zmp1) inhibitor, demonstrates dose-dependent anti-mycobacterial activity against Mtb H37Ra, making it suitable for tuberculosis (TB) research.

(-)-Pinocembrin demonstrates anti-mycobacterial activity against Mycobacterium tuberculosis H37Ra, presenting IC 50 values of 1.11 mg/mL in the dormant phase and 1.21 mg/mL in the active phase. Additionally, this compound exhibits significant antiproliferative effects on various cell lines, including THP-1, A549, Panc-1, HeLa, and MCF7, with IC 50 values ranging from 1.88 to 11.00 mg/mL.

Ermanin, a flavonoid isolated from Tanacetum microphyllum, inhibits platelet aggregation and exhibits anti-tuberculosis, anti-viral bacterial, and potential anti-HIV-1 activities. It has anti-inflammatory properties through the inhibition of iNOS and COX-2 expression and is effective at lower concentrations in inhibiting Dione juno larvae.

BTZ-N3 is an effective and selective anti-tuberculosis drug candidate.

ESAT6 Epitope is a known CD4+ T cell epitope within the Early Secretory Antigenic Target 6 (ESAT6), demonstrating nanoscale affinity (IC50=180 nM) for Major Histocompatibility Complex MHC class I. Additionally, ESAT6 Epitope can enhance the anti-tuberculosis cellular immunity initiated by the Bacille Calmette-Guérin vaccine.

3-Bromoisonicotinic acid, as the most important intermediate among isonicotinic acid derivatives, is mainly used to prepare anti tuberculosis drugs, as well as to synthesize amide, hydrazide, ester and other derivatives.

Dehydrobruceantin has anti-tuberculosis activity.

Antitubercular agent-22 (Compound 2) is an effective antimicrobial agent against Candida albicans MTCC 3017 (MIC: 2.34 μg ml) and M. tuberculosis (H37Rv) (MIC: 2 μg ml).

BM635 is an MmpL3 inhibitor with outstanding anti-mycobacterial activity (MIC50: 0.12 μM against M. tuberculosis H37Rv).

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].

Golotimod hydrochloride (SCV 07 hydrochloride) is an immunomodulating peptide with antimicrobial properties. It enhances antituberculosis therapy effectiveness, promotes thymic and splenic cell proliferation, and boosts macrophage functionality. Furthermore, it inhibits STAT3 signaling, thereby modifying the duration and intensity of oral mucositis in animal models subjected to radiation or a combination of radiation and Cisplatin. Additionally, Golotimod hydrochloride has shown potential as a treatment for recurrent genital herpes simplex virus type 2 (HSV-2) [1] [2] [3].

Lansoprazole sulfide is an impurity of Lansoprazole, which is a gastric pump inhibitor.

Golotimod TFA (SCV 07 TFA) is an immunomodulatory peptide with antibacterial properties that significantly increases the effectiveness of anti-tuberculosis studies, stimulates thymus and splenocyte proliferation and improves macrophage function. Golotimod TFA has the potential to be used in studies of recurrent genital herpes simplex virus type 2 (HSV-2).