659729-85-8

Usage

Uses

Used in Pharmaceutical Industry:
3-Amino-5-hydroxyquinoxalin-2-(1H)-one is used as a therapeutic agent for the treatment of diseases associated with myeloperoxidase (MPO) activity. Its application is based on its capacity to inhibit MPO, thereby reducing oxidative stress and inflammation, which are common in cardiovascular disease, cancer, and neurodegenerative disorders.
Used in Cardiovascular Applications:
In the cardiovascular industry, 3-Amino-5-hydroxyquinoxalin-2-(1H)-one is used as a protective agent to mitigate the effects of oxidative stress and inflammation on the cardiovascular system, potentially reducing the risk of heart diseases.
Used in Oncology:
3-Amino-5-hydroxyquinoxalin-2-(1H)-one is utilized as an anticancer agent, leveraging its MPO-inhibiting properties to combat the oxidative stress and inflammation that contribute to cancer progression.
Used in Neurodegenerative Research:
In the field of neurodegenerative research, 3-Amino-5-hydroxyquinoxalin-2-(1H)-one is employed as a potential therapeutic intervention aimed at reducing the oxidative stress and inflammation implicated in the pathogenesis of neurodegenerative disorders.
Used in Anti-Inflammatory and Antioxidant Therapies:
3-Amino-5-hydroxyquinoxalin-2-(1H)-one is used as an anti-inflammatory and antioxidant agent, capitalizing on its inherent properties to alleviate inflammation and oxidative stress in various conditions.

InChI:InChI=1/C8H7N3O2/c9-7-8(13)10-4-2-1-3-5(12)6(4)11-7/h1-3,12H,(H2,9,11)(H,10,13)

Upstream product

• 659729-79-0 3-amino-5-methoxy-1H-quinoxalin-2-one 

Downstream Products

• 879609-39-9 3-amino-5-(2-chloro-6-(4-(trifluoromethyl)phenyl)pyrimidin-4-yloxy)quinoxalin-2(1H)-one 
• 1085710-78-6 tert-butyl 2-(6-(3-amino-2-oxo-1,2-dihydroquinoxalin-5-yloxy)pyrimidin-4-yl)-5-(trifluoromethyl)phenylcarbamate 
• 1022085-50-2 C₂₄H₂₂F₃N₇O₃ 
• 1022085-51-3 C₂₅H₁₆F₃N₇O₃ 
• 1022085-52-4 C₂₅H₁₆F₃N₇O₃ 

Relevant academic research and scientific papers

Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate

A series of novel 4-oxopyrimidine TRPV1 antagonists was evaluated in assays measuring the blockade of capsaicin or acid-induced influx of calcium into CHO cells expressing TRPV1. The investigation of the structure-activity relationships in the heterocyclic A-region revealed the optimum pharmacophoric elements required for activity in this series and resulted in the identification of subnanomolar TRPV1 antagonists. The most potent of these antagonists were thoroughly profiled in pharmacokinetic assays. Optimization of the heterocyclic A-region led to the design and synthesis of 23, a compound that potently blocked multiple modes of TRPV1 activation. Compound 23 was shown to be effective in a rodent "on-target" biochemical challenge model (capsaicin-induced flinch, ED50 = 0.33 mg/kg p.o.) and was antihyperalgesic in a model of inflammatory pain (CFA-induced thermal hyperalgesia, MED = 0.83 mg/kg, p.o.). Based on its in vivo efficacy and pharmacokinetic profile, compound 23 (N-{4-[6-(4-trifluoromethyl-phenyl)-pyrimidin-4-yloxy]-benzothiazol-2-yl} -acetamide; AMG 517) was selected for further evaluation in human clinical trials.

VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS

Pyrimidine ethers and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

Vanilloid receptor ligands and their use in treatments

Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache,