mycobacterial

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.

Antimycobacterial agent-4 (4-nitro-N-[4-(2-pyridyl)thiazol-2-yl]benzamide) has antibacterial activity against Mycobacterium tuberculosis.

DL-Syringaresinol ( (±)-Syringaresinol) is a lignan from ginseng berries with anti-inflammatory, antioxidant, analgesic and weak anti-mycobacterial activities.DL-Syringaresinol can delay oxidative stress-induced skin aging through autophagy, alleviate oxaliplatin-induced neuropathic pain and sepsis-induced cardiac dysfunction by inhibiting inflammatory responses. neuropathic pain and sepsis-induced cardiac dysfunction by inhibiting inflammatory responses.

MtUng-IN-1 (Compound 18a) inhibits mycobacterial uracil DNA glycosylase (MtUng) with an IC50 value of 300 μM. MtUng-IN-1 is suitable for use in cancer and infectious disease research.

Antimycobacterial agent-2 is an effective anti-mycobacterial agent with a MIC99 of 0.8 μM against Mycobacterium tuberculosis (M.tb) H37Rv. Antimycobacterial agent-2 is cytotoxic, acting on CHO cells (IC50: 48.1 μM).

Antimycobacterial agent-3 is an antimycobacterial agent with low cytotoxicity. antimycobacterial agent-3 is effective against sensitive MTB strain H37Rv and resistant clinical isolates (MIC < 0.029-0.110 μ M).

Antimycobacterial agent-1 (compound 33) demonstrates potent antimycobacterial activity against Mycobacterium tuberculosis H37Ra, with a minimal inhibitory concentration (MIC) value of 1 μg/ml. Notably, antimycobacterial agent-1 exhibits low cytotoxicity in normal cells, as evidenced by an IC50 value of 143.2 μg/ml in Vero cells [1].

Antimycobacterial agent-6 (compound 25) effectively inhibits Mycobacterium tuberculosis, including wild-type and fluoroquinolone-resistant strains, by targeting the Mtb DprE1-C387S mutant. It displays minimal inhibitory concentrations (MIC90) of 0.9 μM for H37Rv and MoxR strains, and 0.5 μM for the DprE1-P116S strain [1].

Bedaquiline (R207910)(TMC207; 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.

Communic acid has antibacterial activity, including against mycobacterial. trans-Communic acid has potential to be utilized as anti-wrinkling agents and cosmetic ingredients, as they suppress UVB-induced MMP-1 expression.

Delamanid D4 is deuterium-labeled Delamanid. Delamanid is a newer mycobacterial cell wall synthesis inhibitor that inhibits the synthesis of mucus acid.

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

Decarine has high antibacterial activity against mycobacterial, gram-positive and gram-negative bacteria, and low cytotoxicity towards human macrophages.Decarine inhibits fMLP/CB-induced elastase release with IC(50) values < or = 5.53 microg/mL.

Dimethyldioctadecylammonium (DDA) is a cationic amphipathic lipid. DDA liposomes containing an Ag85B-ESAT-6 antigen induce antigen deposition at an intramuscular or subcutaneous injection site in mice, increasing immune cell exposure to the antigen. In a guinea pig model of M. tuberculosis infection, spleen bacterial load is reduced and lung and spleen lesion numbers are decreased when the mycobacterial lipid antigens Ac2SGL and PIM2 are administered in liposomes comprised of DDA and a synthetic analog of the mycobacterial cord factor trehalose 6,6-dibehenate (TDB). DDA has also been used in the study of lipid bilayer dynamics.

C-215 is a novel inhibitor of mycobacterial membrane protein large 3 (MmpL3).

(+)-Xylariamide A is a probe used for mycobacterial and fungal carbonic anhydrase.

5,7,3',4'-Tetramethoxyflavone (TMF), a prominent polymethoxyflavone (PMF) derived from M. exotica, displays a range of notable bioactivities. These include anti-malarial, anti-fungal, anti-mycobacterial, and anti-inflammatory properties. Moreover, TMF specifically targets β-catenin signaling to exhibit chondroprotective activity.

ONX-0914 (PR-957) TFA is a selective, noncompetitive, irreversible inhibitor targeting the chymotrypsin-like subunit (LMP7) of the immunoproteasome, effectively blocking cytokine production and mitigating the progression of experimental arthritis. With a K_i value of 5.2 μM against the mycobacterial proteasome, ONX-0914 TFA also facilitates the reactivation of latent HIV-1 by inducing p-TEFb activation through HSF-1 mediation [1] [2] [3].

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).

DprE1-IN-6 (Compound 56) is a DprE1 inhibitor with demonstrated anti-TB activity, exhibiting a minimum inhibitory concentration (MIC) of 1 μM against the Mtb H37Rv strain, along with efficacy against drug-resistant mycobacterial strains. Moreover, it possesses high microsomal stability and medium clearance [1].

1.(-)-Licarin B (Licarine B) has anti-mycobacterial activity.

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

Norverapamil hydrochloride (D591 hydrochloride) ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

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].

Antibacterial agent 118 (also known as compound 20) is a potent antimycobacterial compound with activity against various mycobacterial strains, including Mtb H37Ra, M. aurum, M. smegmatis, Mtb H37Rv, and M. avium. The minimum inhibitory concentration (MIC) values for Antibacterial agent 118 against these strains are 40.7 μM, 10.2 μM, 163.0 μM, 62.5 μM, and 62.5 μM, respectively. This compound holds potential for tuberculosis research [1].

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

Antibacterial agent 121 (Compound 10) demonstrates antibacterial properties and exhibits efficacy against mycobacterial strains while also possessing anti-inflammatory activity. This compound finds potential applications in Tuberculosis (TB) research [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].

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

(-)-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.

Calcimycin (A-23187) is an ionophorous, polyether carboxylic antibiotic from Streptomyces chartreusensis. It binds and transports calcium and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.

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].

Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavone II may have therapeutic potential for the treatment of allergic asthma.Skullcapflavone II regulates osteoclast differentiation, survival, and function. Skullcapflavone II exerts potent antimicrobial activity against M. aurum and M. bovis BCG

Antibacterial agent 122 (compound 15) is a thiourea derivative that can be used in the studies of tuberculosis. Antibacterial agent 122 shows low cytotoxicity as well as anti-mycobacterial activity [1].

PknB-IN-1 (Compound 2) is an inhibitor of protein kinase B (PknB) with a concentration causing 50% inhibition (IC50) of 14.4 μM. This compound demonstrates anti-mycobacterial activity by effectively suppressing the growth of M. tuberculosis H37Rv strain, with a minimum inhibitory concentration (MIC) of 6.2 μg/mL [1].

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.