3-Hydrazino-quinoxaline-2-thiol

Product Name3-Hydrazino-quinoxaline-2-thiol
CAS13080-21-2
MFC8H8N4S
MW192.24
EINECS
MOL File13080-21-2.mol

Chemical Properties

Melting point	254 °C (decomp)(Solv: ethanol (64-17-5))
Boiling point	376.1±25.0 °C(Predicted)
Density	1.55±0.1 g/cm3(Predicted)
pka	7.91±0.20(Predicted)
form	Solid
color	Light yellow to yellow

Usage And Synthesis

Uses

HPi1 is a potent, selective and orally active antimicrobial against Helicobacter pylori with an IC50 of 0.24 μM and an MIC of 0.08-0.16 μg/mL. HPi1 is inactive against other bacteria, including the gut commensals Lactobacillus casei, Lactobacillus reuteri, and Bifidobacterium longum[1].

Biological Activity

HPi1 is a potent, selective and orally active antibacterial agent against Helicobacter pylori with IC50 of 0.24 μM and MIC of 0.08-0.16 μg/mL. It is inactive against other bacteria, including the enteric bacteria Lactobacillus casei, Lactobacillus reuteri and Bifidobacterium longum.

in vitro

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.

in vivo

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^[1].

Animal Model:	Adult specific-pathogen-free female C57BL/6 mice (6-8-week-old) fed with H. pylori SS1 suspension^[1]
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.

target

IC50: 0.24 μM ( Helicobacter pylori )
MIC: 0.08-0.16 μg/mL ( Helicobacter pylori )

References

[1] Gavrish E, et al. In vitro and in vivo activities of HPi1, a selective antimicrobial against Helicobacter pylori. Antimicrob Agents Chemother. 2014 Jun;58(6):3255-60. DOI:10.1128/AAC.02573-13

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