3-肼基喹喔啉-2(1H)-硫酮
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- CAS号:
- 13080-21-2
- 英文名:
- 3-HYDRAZINO-QUINOXALINE-2-THIOL
- 英文别名:
- AKOS BBS-00008251;CHEMBRDG-BB 5215319;3-HYDRAZINO-QUINOXALINE-2-THIOL;3-Hydrazinylquinoxaline-2-thiol;3-Hydrazinylquinoxaline-2(1H)-thione;2(1H)-Quinoxalinethione, 3-hydrazinyl-;3-hydrazinoquinoxaline-2-thiol(SALTDATA: FREE);membranes,Helicobacter,ulcer,Antimicrobial,gastric,HPi1,inhibit,Inhibitor,Bacterial,permeate,HPi 1,HPi-1,orally,pylori,peptic
- 中文名:
- 3-肼基喹喔啉-2(1H)-硫酮
- 中文别名:
- 化合物HPI1;3-肼基喹喔啉-2(1H)-硫酮
- CBNumber:
- CB1135666
- 分子式:
- C8H8N4S
- 分子量:
- 192.24
- MOL File:
- 13080-21-2.mol
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3-肼基喹喔啉-2(1H)-硫酮化学性质
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熔点:
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254 °C (decomp)(Solv: ethanol (64-17-5))
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沸点:
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376.1±25.0 °C(Predicted)
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密度:
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1.55±0.1 g/cm3(Predicted)
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酸度系数(pKa):
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7.91±0.20(Predicted)
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形态:
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Solid
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颜色:
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Light yellow to yellow
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3-肼基喹喔啉-2(1H)-硫酮性质、用途与生产工艺
HPi1 是一种针对幽门螺杆菌 (Helicobacter pylori) 的有效，选择性和具有口服活性的抗菌剂，IC50 为 0.24 μM，MIC 为 0.08-0.16 μg/mL。HPi1 对其他细菌无活性，包括肠道菌干酪乳杆菌，罗伊氏乳杆菌和长双歧杆菌。
IC50: 0.24 μM (
Helicobacter pylori
)
MIC: 0.08-0.16 μg/mL (
Helicobacter pylori
)
The MIC against
H. pylori
isolates ranged from 0.002-0.032 μg/mL (0.01-0.17 μM) in the agar dilution assay. HPi1 is effective against the clarithromycin-resistant strains ARHp172 (MIC of 0.004–0.016 μg/mL) and ARHp246 (MIC of 0.008–0.032 μg/mL).
HPi1 has some activity against the
Bacteroides species
, but at concentrations at least 18-fold higher than the
H. pylori
MIC. More potent activity is detected for
Campylobacter jejuni
with an MIC of 0.3 μg/mL.
HPi1 has good physicochemical and pharmacological properties, including determining the aqueous solubility (19 μg/mL), human plasma protein binding (93% bound), stability with human liver microsomes (T
1/2
of 1.3 hours) and the ability to passively permeate membranes.
HPi1 (6.25-50 mg/kg; Oral gavage; once a day; for 3 days; female C57BL/6 mice) treatment decreases colony counts below the limit of detection at doses of 25 or 50 mg/kg/day.
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Animal Model:
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Adult specific-pathogen-free female C57BL/6 mice (6-8-week-old) fed with
H. pylori
SS1 suspension
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Dosage:
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6.25 mg/kg, 12.5 mg/kg, 25 mg/kg, 50 mg/kg
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Administration:
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Oral gavage; once a day; for 3 days
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Result:
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Reduced colony counts to below the limit of detection.
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3-肼基喹喔啉-2(1H)-硫酮
上下游产品信息
上游原料
下游产品
13080-21-2, 3-肼基喹喔啉-2(1H)-硫酮 相关搜索:
- 抑制剂
- 化合物HPI1
- 3-肼基喹喔啉-2(1H)-硫酮
- 13080-21-2
- membranes,Helicobacter,ulcer,Antimicrobial,gastric,HPi1,inhibit,Inhibitor,Bacterial,permeate,HPi 1,HPi-1,orally,pylori,peptic
- 2(1H)-Quinoxalinethione, 3-hydrazinyl-
- 3-Hydrazinylquinoxaline-2-thiol
- 3-Hydrazinylquinoxaline-2(1H)-thione
- 3-hydrazinoquinoxaline-2-thiol(SALTDATA: FREE)
- 3-HYDRAZINO-QUINOXALINE-2-THIOL
- AKOS BBS-00008251
- CHEMBRDG-BB 5215319