Isoniazid

Isoniazid (Isonicotinic hydrazide) is an antibacterial agent used primarily as a tuberculostatic.

high affinity agonist of the translocator protein

Isoniazid pyruvate is a metabolite of isoniazid. Isoniazid (Laniazid, Nydrazid), also known as isonicotinylhydrazine (INH), is an organic compound that is the first-line medication in prevention and treatment of tuberculosis.

Isoniazid-D4 is a deuterium isotope marker for Isoniazid (TMSM-1385), which can be used for isotope tracing and drug metabolism studies.Isoniazid is a prodrug that must be activated by the bacterial peroxidase KatG, and is bactericidal against rapidly dividing Mycobacterium species.

Isoniazid (Standard) is the standard substance of Isoniazid, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Isoniazid (Isonicotinic hydrazide) is an antibacterial agent used primarily as a tuberculostatic.

Isoniazid-D4 (Standard) is a reference standard of Isoniazid-D4 intended for quantitative analysis, quality control, and related biochemical research applications. Isoniazid-d4 is a deuterium isotope marker for Isoniazid, which can be used for isotope tracing and drug metabolism studies.Isoniazid is a prodrug that must be activated by the bacterial peroxidase KatG, and is bactericidal against rapidly dividing Mycobacterium species.

Acetyl-Isoniazid-[D4] (Standard) is a reference standard of Acetyl-Isoniazid-[D4] intended for quantitative analysis, quality control, and related biochemical research applications.

Isoniazid-KLH is a hapten–carrier protein conjugate generated by chemically coupling Isoniazid to keyhole limpet hemocyanin (KLH), in which Isoniazid acts as a low-molecular-weight hapten that cannot induce an immune response on its own and must be conjugated to a macromolecular carrier protein to become immunogenic, thereby enabling its use in antibody generation, immunological detection systems, and experimental studies focused on drug-specific immune recognition and assay development.

Isoniazid-BSA is a hapten-carrier protein conjugate formed by binding isoniazid to BSA (bovine serum albumin). It enhances isoniazid-induced immune responses by combining a hapten with a protein adjuvant, commonly used in vaccine or antibody preparation research.

Acetylisoniazid (Standard) is a reference standard for research and analysis in studies involving Acetylisoniazid. Acetylisoniazid is a metabolite of Isoniazid, formed through the catalysis of N-acetyltransferase (NAT). Isoniazid exhibits bactericidal properties against rapidly dividing mycobacteria and possesses antitubercular activity.

Acetylisoniazid is a metabolite of Isoniazid, formed through the catalysis of N-acetyltransferase (NAT). Isoniazid exhibits bactericidal properties against rapidly dividing mycobacteria and possesses antitubercular activity.

Isonicotinic acid, a metabolite of isoniazid and a useful isomer of nicotinic acid, is formed from isoniazid by hydrazinolysis and can be catalyzed by cytochrome P450 enzymes, such as CYP2C.

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

Mtb-IN-6 (Compound C10) is a Mycobacterium tuberculosis (Mtb) respiratory inhibitor. It enhances the bactericidal activity of isoniazid (INH) and inhibits wild-type Mtb with an IC50 of 25 µM.

UH-NIP-16 exhibits antibacterial activity against Mycobacterium tuberculosis, effectively inhibiting the pathogenic mycobacterium strains H37Rv and CDC1551 with MIC50 values of 1.86 and 3.05 μM, respectively. Additionally, UH-NIP-16 synergistically enhances the antitubercular effects when used with antituberculosis agents such as Streptomycin, Isoniazid, Ethambutol, and Bedaquiline.

NADH-IN-3 (Compound C4-1) is an NADH inhibitor with a minimum inhibitory concentration (MIC) of 4 μg/mL (13.042 μM) against the type II NADH dehydrogenase of Mycobacterium tuberculosis (Mtb). It effectively blocks ATP synthesis and demonstrates potent inhibitory effects on both single-drug (Rifampicin and Isoniazid) and multidrug-resistant (Mtb) strains, exhibiting antibacterial activity while maintaining low cytotoxicity towards HepG2 cells (SI: 16.52).

Antimycobacterial agent-12 (Compound Ec42) is a Platensimycin derivative and acts as a dual inhibitor of KasA and KasB. It demonstrates minimum inhibitory concentrations (MIC) of 2 μg/mL against Staphylococcus aureus ATCC 29213, 2 μg/mL against Mycobacterium smegmatis, and 4 μg/mL against its isoniazid-resistant strains. In a Mycobacterium smegmatis-infected mouse model, Antimycobacterial agent-12 exhibits excellent antimycobacterial activity, making it a valuable tool for tuberculosis research.

β-Defensin-1 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth ofB. adolescentis,L. acidophilus,B. breve,B. vulgatus,L. fermentum,B. longum, andS. thermophilusin an antimicrobial radial diffusion assay.2β-Defensin-1 also inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius, and of susceptibleM. tuberculosisH37Rv but not of resistantM. tuberculosisRM22 when used at a concentration of 128 μg/ml.3,4It blocks human and mouse Kv1.3 voltage-gated potassium channels (IC50s = 11.8 and 13.2 μM, respectively).5Overexpression of β-defensin-1 in the human oral squamous cell carcinoma (OSCC) cell lines HSC-3, UM-1, and SCC-9 increases migration and invasion but not proliferation.6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Schroeder, B.O., Ehmann, D., Precht, J.C., et al.Paneth cell α-defensin 6 (HD-6) is an antimicrobial peptideMucosal Immunol.8(3)661-671(2015) 3.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 4.Fattorini, L., Gennaro, R., Zanetti, M., et al.In vitro activity of protegrin-1 and beta-defensin-1, alone and in combination with isoniazid, against Mycobacterium tuberculosisPeptides25(7)1075-1077(2004) 5.Feng, J., Xie, Z., Yang, W., et al.Human beta-defensin 1, a new animal toxin-like blocker of potassium channelToxicon113(2016) 6.Han, Q., Wang, R., Sun, C., et al.Human beta-defensin-1 suppresses tumor migration and invasion and is an independent predictor for survival of oral squamous cell carcinoma patientsPLoS One9(3)e91867(2014)

Linoleoyl-L-carnitine chloride is a long-chain acylcarnitine and an endogenous intermediate in fatty acid metabolism.

Pyridomycin is a structurally unusual antimycobacterial cyclodepsipeptide whose composition includes two rare moieties: 3-(3-pyridyl)-L-alanine and 2-hydroxy-3-methylpent-2-enoic acid. It inhibits NADH-dependent enoyl (Acyl-Carrier-Protein) reductase InhA, preventing mycolic acid synthesis in M. tuberculosis, including isoniazid-resistant strains (MICs = 0.31-0.63 μg/ml).

OPC-167832 is a highly potent and orally bioavailable dprE1 inhibitor with an IC₅₀ of 0.258 μM. It exhibits anti-mycobacterial activity against Mycobacterium tuberculosis and can be used in tuberculosis-related research.

Thiocarlide (isoxyl) is a thiourea derivative that was used in the 1960s to successfully treat tuberculosis (TB). It has considerable antimycobacterial activity in vitro and is effective against multi-drug resistant strains of Mycobacterium tuberculosis in the range of 1-10 µg/ml. [1] [2] At concentrations of 10 µM, isoxyl inhibits the synthesis of M. bovis during six hours of exposure which is similar to isoniazid (INH) and ethionamide (ETH), two other predominant anti-tuberculosis drugs. Unlike INH and ETH, isoxyl also partially inhibits the synthesis of fatty acids. Isoxyl shows no acute toxicity against primary macrophage cell cultures as demonstrated by diminution of redox activity.[2]

Mtb-IN-4 (compound 17h) is a non-toxic isoxazole that exhibits anti-Mycobacterium tuberculosis (Mtb) activity with an IC50 value of 0.70 μM. It impedes Mtb respiration and biofilm formation within macrophages and augments the efficacy of the antibiotic isoniazid (INH) against INH-resistant Mtb mutants [1].

Mtb-IN-5 (compound (-)17j) is an isoxazole with anti-Mycobacterium tuberculosis (Mtb) activity, inhibiting Mtb respiration and biofilm formation within macrophages, and enhancing the efficacy of the antibiotic isoniazid (INH) against INH-resistant Mtb mutants [1].