The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases was written by Brown, Dearg S.;Cumming, John G.;Bethel, Paul;Finlayson, Jonathan;Gerhardt, Stefan;Nash, Ian;Pauptit, Richard A.;Pike, Kurt G.;Reid, Alan;Snelson, Wendy;Swallow, Steve;Thompson, Caroline. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Related Products of 14678-05-8 This article mentions the following:
A novel, potent and selective quinazolinone series of inhibitors of p38α MAP kinase has been identified. Modifications designed to address the issues of poor aqueous solubility and high plasma protein binding as well as embedded aniline functionalities resulted in the identification of a clin. candidate N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703). Optimization was guided by understanding of the binding modes from X-ray crystallog. studies which showed a switch from DFG out’ to DFG in’ as the inhibitor size was reduced to improve overall properties. In the experiment, the researchers used many compounds, for example, Isoxazol-5-amine (cas: 14678-05-8Related Products of 14678-05-8).
Isoxazol-5-amine (cas: 14678-05-8) belongs to isoxazole derivatives. Isoxazoles are aromatic heterocycles containing an N–O bond. The weakness of this bond allows the ring opening of these heterocycles under reductive conditions. The most common methods for N–O bond cleavage in isoxazoles are hydrogenation with palladium or platinum catalysts or with Raney Ni. Recent developments have shown that Mo(CO)6 efficiently cleaves the N–O bond in isoxazoles.Related Products of 14678-05-8
Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem