659730-14-0

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General Description

2-amino-8-hydroxyquinazolin is a chemical compound that belongs to the quinazoline family and consists of a quinazoline ring with an amino group at the 2-position and a hydroxy group at the 8-position. It is a heterocyclic compound with potential pharmaceutical applications, particularly in the field of medicinal chemistry. 2-amino-8-hydroxyquinazolin has been studied for its diverse biological activities, including its potential as an antitumor agent and its ability to inhibit certain enzymes. Additionally, its unique structure and properties make it a valuable building block in the synthesis of pharmaceuticals and other organic molecules. Overall, 2-amino-8-hydroxyquinazolin is a versatile and important chemical compound with potential applications in various areas of science and medicine.

Upstream product

• 708-15-6 2-amino-8-methoxyquinazoline 
• 70127-96-7 2-amino-3-methoxy-benzaldehyde 
• 53055-05-3 3-methoxy 2-nitrobenzaldehyde 

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.