helicobacter

HPi1 is a selective and orally active antimicrobial against Helicobacter pylori (IC50: 0.24 μM and a MIC of 0.08-0.16 μg/mL). HPi1 is inactive against other Xaliproden, including the gut commensals, Lactobacillus reuteri, Lactobacillus casei, and Bifidoba

CV-6209 is a potent antagonist of the platelet-activating factor (PAF) receptor.

pNNP (Nitrophenylphosphate) can be used as a substrate for the PP2C assay. pNNP inhibits β-carbonic anhydrase and α-carbonate dehydrogenase, as well as H. pylori Helicobacter pylori. pNNP is a weakly active, tissue-nonspecific alkaline phosphatase modifier. pNNP has been shown to inhibit β-carbonic anhydrase and α-carbonate dehydrogenase.

L-Glutamic acid monosodium salt monohydrate (MSG monohydrate) is an important food additive with gastrointestinal protective effects. It plays a critical role in nutrient metabolism, energy demand, immune response, oxidative stress, signal transduction, and synaptic transmission. L-Glutamic acid monosodium salt monohydrate can induce oxidative stress, DNA damage, and apoptosis in mouse liver and brain tissues. It can protect against gastrointestinal damage caused by NSAIDs and Helicobacter pylori through multiple mechanisms.

Finafloxacin, a fluoroquinolone antimicrobial agent from a new 8-cyano subclass, is most effective in slightly acidic environments (pH 5.0-6.0), a condition where other fluoroquinolones typically reduce in activity. It selectively targets bacterial type II topoisomerases, such as DNA gyrase and DNA topoisomerase IV, making it suitable for treating serious bacterial infections particularly in acidic contexts, including urinary tract infections (UTIs) and Helicobacter pylori infections.

FR-145715 is a histamine H2 receptor antagonist characterized by its specific anti-Helicobacter pylori activity. This compound is utilized in the study of gastric lesions.

JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg mL. It shows affinity for binding to H+ K+-ATPase, COX-1 2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.

BAS-118 is a benzamide derivative exhibiting antibacterial activity. For 100 randomly selected strains of Helicobacter pylori, its MIC50, MIC90, and MIC range were ≤0.003, 0.013, and ≤0.003-0.025 mg L, respectively. BAS-118 shows potential for research as an anti-H. pylori agent.

Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori), with an IC50 of 0.14 μM for H. pylori inhibition. It effectively decreases apoptosis in GES-1 cells infected with H. pylori and reduces levels of ROS and γH2AX. Urease-IN-20 also demonstrates significant gastric mucosal protective effects, making it suitable for H. pylori research.

Urease-IN-12 (compound 5e) is a competitive urease inhibitor with an IC50 of 0.35 μM, showing potential in inhibiting gastritis and peptic ulcers caused by Helicobacter pylori.

Antibacterialagent 231 (derivative 8) is an antimicrobial compound effective against multidrug-resistant Helicobacter pylori (H. pylori), with a minimum inhibitory concentration ranging from 0.25 to 0.5 μg/mL. It specifically targets the protein translocase subunit SecA and the outer membrane protein assembly factor BamD to inhibit the transport and assembly of bacterial outer membrane proteins (OMPs). Antibacterialagent 231 is suitable for studying the effects of antibiotic treatment on gut microbiome balance.

FR-182024 is a novel cephem derivative, it has potent anti-Helicobacter pylori activity.

MDK-4624 is a AMPKα1 activator. MDK-4624 inhibits Helicobacter pylori-induced oxidative stresses and gastric epithelial cell apoptosis. MDK-4624 attenuates dexamethasone-induced osteoblast cell death. MDK-4624 potently inhibits melanoma cell proliferation

Spirolaxine, a natural product isolated from Sporotrichum laxum ATCC 15155, has shown a variety of biological activities including promising anti-Helicobacter pylori property.

4-Amino-6-chloro-1,3-benzenedisulfonamide is a carbonic anhydrase inhibitor.1 Formulations containing this compound are diuretics.2 4-Amino-6-chloro-1,3-benzenedisulfonamide is detected as a hydrolysis product of chlorothiazide in the urine.2 Diuretics, including chlorothiazide, have been abused as performance-enhancing drugs and masking agents in sports doping.3References1. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).2. Deventer, K., Pozo, O.J., Van Eenoo, P., et al. Detection of urinary markers for thiazide diuretics after oral administration of hydrochlorothiazide and altizide-relevance to doping control analysis. J. Chromatogr. A 1216(12), 2466-2473 (2009).3. Cadwallader, A.B., de la Torre, X., Tieri, A., et al. The abuse of diuretics as performance-enhancing drugs and masking agents in sport doping: Pharmacology, toxicology and analysis. Br. J. Pharmacol. 161(1), 1-16 (2010). 4-Amino-6-chloro-1,3-benzenedisulfonamide is a carbonic anhydrase inhibitor.1 Formulations containing this compound are diuretics.2 4-Amino-6-chloro-1,3-benzenedisulfonamide is detected as a hydrolysis product of chlorothiazide in the urine.2 Diuretics, including chlorothiazide, have been abused as performance-enhancing drugs and masking agents in sports doping.3 References1. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).2. Deventer, K., Pozo, O.J., Van Eenoo, P., et al. Detection of urinary markers for thiazide diuretics after oral administration of hydrochlorothiazide and altizide-relevance to doping control analysis. J. Chromatogr. A 1216(12), 2466-2473 (2009).3. Cadwallader, A.B., de la Torre, X., Tieri, A., et al. The abuse of diuretics as performance-enhancing drugs and masking agents in sport doping: Pharmacology, toxicology and analysis. Br. J. Pharmacol. 161(1), 1-16 (2010).

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (40 mg/kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

Cholesterol β-D-Glucoside (β-D-Glucopyranoside) is a toxicant produced by the human parasite Helicobacter pylori.

Lacto-N-biose I, also known as Galβ1-3GlcNAc, is a naturally occurring metabolite that serves as a substrate for the α1,2-fucosyltransferase enzyme derived from Helicobacter pylori[1].

Licoricone exhibits anti-helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains.

Antofloxacin is a well-tolerated, orally active, and broad-spectrum 8-amino-fluoroquinolone compound that exhibits potent antibacterial properties. It demonstrates superior activity against gyrA mutation-positive Helicobacter pylori strains, particularly in strains with mutations in the Asn87 position, when compared to levofloxacin. Additionally, Antofloxacin acts as a weak but reversible inhibitor of CYP1A2 and is clinically used to treat infections caused by various bacterial species.

Ecabet sodium (TA-2711) is a chemical compound utilized for the clinical treatment of gastrointestinal disease through the suppression of reactive oxygen species (ROS) generation and enhancement of Helicobacter pylori eradication [1]. Moreover, Ecabet sodium effectively attenuates apoptosis [2].

Vonoprazan hydrochloride, a proton pump inhibitor (PPI), effectively functions as a potassium-competitive acid blocker (P-CAB) with potent antisecretory properties. It significantly inhibits H+,K+-ATPase activity in porcine gastric microsomes, displaying an IC50 of 19 nM at pH 6.5. Developed primarily for researching acid-related conditions such as gastroesophageal reflux disease and peptic ulcer disease, vonoprazan hydrochloride also aids in the eradication of Helicobacter pylori [1] [2] [3].

Bismuth Subcitrate Potassium is an antibiotic that acts against 12 species of Helicobacter pylori, inhibits the histamine H2 receptor, and can be used to study diarrhea and peptic ulcer disease in vulnerable patients with SARS-CoV-2 infections.

Ranitidine bismuth citrate, an orally administered Histamine H2-receptor antagonist, demonstrates a potent inhibitory concentration (IC 50) of 3.3 μM and exhibits high selectivity towards SARS-CoV-2-infected cells. It is widely utilized as an anti-Helicobacter pylori agent, exhibiting a minimum inhibitory concentration (MIC 90) value of 16 ng/L.