3-HYDRAZINO-QUINOXALINE-2-THIOL
3-HYDRAZINO-QUINOXALINE-2-THIOL Basic information
- Product Name:
- 3-HYDRAZINO-QUINOXALINE-2-THIOL
- Synonyms:
-
- CHEMBRDG-BB 5215319
- AKOS BBS-00008251
- 3-HYDRAZINO-QUINOXALINE-2-THIOL
- 3-hydrazinoquinoxaline-2-thiol(SALTDATA: FREE)
- 2(1H)-Quinoxalinethione, 3-hydrazinyl-
- 3-Hydrazinylquinoxaline-2-thiol
- 3-Hydrazinylquinoxaline-2(1H)-thione
- membranes,Helicobacter,ulcer,Antimicrobial,gastric,HPi1,inhibit,Inhibitor,Bacterial,permeate,HPi 1,HPi-1,orally,pylori,peptic
- CAS:
- 13080-21-2
- MF:
- C8H8N4S
- MW:
- 192.24
- Mol File:
- 13080-21-2.mol
3-HYDRAZINO-QUINOXALINE-2-THIOL 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
3-HYDRAZINO-QUINOXALINE-2-THIOL Usage And Synthesis
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.
target
IC50: 0.24 μM ( Helicobacter pylori )
MIC: 0.08-0.16 μg/mL ( Helicobacter pylori )
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