3-肼基喹喔啉-2(1H)-硫酮
3-肼基喹喔啉-2(1H)-硫酮 性质
| 熔点 | 254 °C (decomp)(Solv: ethanol (64-17-5)) |
|---|---|
| 沸点 | 376.1±25.0 °C(Predicted) |
| 密度 | 1.55±0.1 g/cm3(Predicted) |
| 酸度系数(pKa) | 7.91±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
3-肼基喹喔啉-2(1H)-硫酮 用途与合成方法
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.
| Animal Model: | Adult specific-pathogen-free female C57BL/6 mice (6-8-week-old) fed with H. pylori SS1 suspension |
| Dosage: | 6.25 mg/kg, 12.5 mg/kg, 25 mg/kg, 50 mg/kg |
| Administration: | Oral gavage; once a day; for 3 days |
| Result: | Reduced colony counts to below the limit of detection. |
