33443-53-7

Usage

InChI:InChI=1/C14H9BrN2O/c15-10-6-7-12-11(8-10)13(17-14(18)16-12)9-4-2-1-3-5-9/h1-8H,(H,16,17,18)

Upstream product

• 108-86-1 bromobenzene 
• 39263-32-6 2-amino-5-bromobenzonitrile 
• 79-22-1 methyl chloroformate 
• 541-41-3 chloroformic acid ethyl ester 
• 100-58-3 phenylmagnesium bromide 
• 39859-36-4 2-amino-5-bromobenzophenone 
• 57-13-6 urea 

Relevant academic research and scientific papers

Novel 1,2-dihydroquinazolin-2-ones: Design, synthesis, and biological evaluation against Trypanosoma brucei

In 2014, a published report of the high-throughput screen of?>42,000 kinase inhibitors from GlaxoSmithKline against T. brucei identified 797 potent and selective hits. From this rich data set, we selected NEU-0001101 (1) for hit-to-lead optimization. Through our preliminary compound synthesis and SAR studies, we have confirmed the previously reported activity of 1 in a T. brucei cell proliferation assay and have identified alternative groups to replace the pyridyl ring in 1. Pyrazole 24 achieves improvements in both potency and lipophilicity relative to 1, while also showing good in vitro metabolic stability. The SAR developed on 24 provides new directions for further optimization of this novel scaffold for anti-trypanosomal drug discovery.

Biomimetic Asymmetric Reduction of Quinazolinones with Chiral and Regenerable NAD(P)H Models

A facile approach to chiral dihydroquinazolinone derivatives has been described via biomimetic asymmetric reduction of quinazolinones with chiral and regenerable NAD(P)H models. The utility of this method was demonstrated by a concise synthesis of the bromodomain protein divalent inhibitor.

Microwave assisted synthesis of 4-phenylquinazolin-2(1H)-one derivatives that inhibit vasopressor tonus in rat thoracic aorta

Quinazolinones have pharmacological effects on vascular reactivity through different mechanisms. We synthesized 4-phenylquinazolin-2(1H)-one derivatives under microwave irradiation and tested them on the rat thoracic aorta. The prepared compounds 2a-2f were obtained in about 1 h with suitable yields (31-92%). All derivatives produced vasorelaxant effects with IC50 values ranging from 3.41 ± 0.65 μM to 39.72 ± 6.77 μM. Compounds 2c, 2e and 2f demonstrated the highest potency in endothelium-intact aorta rings (IC50 4.31 ± 0.90 μM, 4.94 ± 1.21 μM and 3.41 ± 0.65 μM respectively), and they achieved around 90% relaxation (30 μM). In aorta rings without an endothelium, the effect of compound 2f was abolished. Using the MTT assay to test for cell viability, only compound 2b induced cytotoxicity at the maximum concentration employed (30 μM). The results show that vasorelaxation by 4-phenylquinazolin-2(1H)-one derivatives might depend on the activation of a signalling pathway triggered by endothelium-derived factors.

SUBSTANCE CAPABLE OF INHIBITING CYTOKININ SIGNALING

Disclosed are: a substance which has an activity of inhibiting the intracellular signaling from a plant-derived cytokinin receptor and which can control the growth or differentiation of a plant. Also, disclose is a method for searching for a chemical subs

SYNTHESIS OF QUINAZOLINES

Grignard reagents reacted with 2-aminobenzonitrile to give the intermediate (10), which readily could be cyclized to quinazolines by reaction with carbonyl compounds (e.g. acid chlorides, anhydrides, formates and oxalates).The intermediate (10) and aldehy

Production of quinazolinone compounds

2(1H)-Quinazolinone derivatives, which are useful as anti-inflammatory agents, are prepared by heating or hydrolyzing an acylurea derivative. The acylurea derivative can be prepared by either reacting an indole derivative with an oxidizing agent or reacti