helicobacter

HPi1 是一种有口服活性的，针对幽门螺杆菌的选择性抗菌剂，IC50为 0.24 μM，MIC 为 0.08-0.16 μg mL。

CV-6209 是一种具有选择性和高效性的血小板活化因子 (PAF) 拮抗剂，具有抗增殖作用，部分抑制乙酰胆碱诱导的低血压，抑制 Paf 诱导的 PMN 或血小板聚集。CV-6209 具有抗幽门螺杆菌作用，可以抑制 PAF 引起的大鼠低血压。

pNNP (Nitrophenylphosphate) 可用作 PP2C 试验的底物。pNNP 对β-碳酸酐酶和α-碳酸酯脱水酶有抑制作用，对幽门螺杆菌幽门螺杆菌也具有抑制作用。pNNP 是一种活性较弱的组织非特异性碱性磷酸酶调节剂。

L-Glutamic acid monosodium salt monohydrate （MSG monohydrate）是一种重要的食品添加剂，具有胃肠道保护作用，在营养代谢、能量需求、免疫响应、氧化应激、信号通路调节及突触传递中有重要作用。L-Glutamic acid monosodium salt monohydrate 诱导小鼠肝脏和脑组织氧化应激、DNA损伤和细胞凋亡。L-Glutamic acid monosodium salt monohydrate 可通过多种机制保护非甾体抗炎药及幽门螺杆菌引起的胃肠道损伤。

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 作为一种组胺H2受体拮抗剂，展现出针对幽门螺杆菌的特异性抗菌活性，常用于研究胃部病变。

JAK05 对 Helicobacter pylori 具有抑制活性，能抑制 J63、J196 和 J107 菌株，其最低抑制浓度（MIC）为 3-5 µg mL。JAK05 对 H+ K+-ATPase、COX-1 2、TNF-α 和 PGE2 具有结合亲和力，具备抗氧化及抗炎特性。该化合物在大鼠乙醇诱发的胃溃疡模型中显示出抗溃疡活性。

BAS-118 是一种具有抗菌活性的苯酰胺衍生物。在对 100 株随机选择的幽门螺杆菌(Helicobacter pylori) 分离株的测试中，其MIC50、MIC90和MIC范围分别为 ≤0.003、0.013 和 ≤0.003-0.025 mg L。BAS-118 有潜力用于抗H. pylori剂的研究。

Urease-IN-20 (compound XBP2) 是一种针对 Helicobacter pylori (H. pylori) 的抑制剂，具有 0.14 μM 的 IC50。在感染 H. pylori 的 GES-1 细胞中，Urease-IN-20 能减少细胞凋亡 (Apoptosis) 和降低 ROS 与 γH2AX 的水平。它展示了显著的胃黏膜保护作用，适用于幽门螺杆菌研究。

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) 是由人类寄生虫幽门螺杆菌产生的毒性物质。

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 是一种高效且具口服活性的质子泵抑制剂 (PPI) 和钾竞争性酸阻断剂 (potassium-competitive acid blocker, P-CAB)，展示出优秀的抗分泌活性。在 pH 为 6.5 的条件下，该化合物可抑制猪胃微粒体内 H+,K+-ATPase 的酶活性，呈现出 19 nM 的 IC50 值。Vonoprazan hydrochloride 主要应用于胃酸相关疾病的研究，包括胃食管反流病和消化性溃疡，并可用于根除幽门螺杆菌。

Bismuth Subcitrate Potassium 是一种对 12 种幽门螺杆菌有作用的抗生素，抑制组胺H2受体，可用于研究 SARS-CoV-2 感染脆弱患者的腹泻和消化性溃疡病。

Ranitidine bismuth citrate 为一种口服活性的组胺H2受体(Histamine H2-receptor)拮抗剂，其IC50值为3.3 μM，对SARS-CoV-2感染细胞显示高选择性。该化合物还是治疗幽门螺杆菌(Helicobacter Pylori)感染的常用试剂，其MIC90为16 ng L。

alpha-1,3 4-Fucosyltransferase (α1,3 4FucT) (Hp3 4FT) 存在于幽门螺杆菌中。alpha-1,3 4-Fucosyltransferase (α1,3 4FucT) 催化岩藻糖从供体 GDP-β-l-岩藻糖转移到 GlcNAc。

1-Methyl-2-(8E)-8-tridecenyl-4(1H)-quinolinone 对幽门螺杆菌菌株 51 表现出有效的抗菌活性，MIC50 值和 MIC90 值分别为 22 µM 和 50 µM。该化合物展现了在研究胃及十二指肠溃疡方面的潜力。