19795-35-8Relevant academic research and scientific papers
Heterocyclic compounds from 4H-3,1-benzoxazin-4-one derivatives as anticancer agent
Abdel-Rahman, Taha M.
, p. 1257 - 1265 (2005)
Behaviour of 2-(4-oxo-4H-benzo[d][1,3]oxazin-2-yl)-benzoic acid (1) towards nitrogen nucleophiles namely, hydrazine hydrate, in different solvents, ammonium acetate, and o-phenylenediamine has been investigated to give aminoquinazolin-4-one, benzotriazepi
Regiospecific Isomerization of 2-Benzoxazinon-2-yl Benzoic Acid Toward Some Nitrogen Nucleophiles as Environmental Insecticide
El-Hashash, Maher A.,Rizk, Sameh A.,El-Naggar, Abeer M.,El-Bana, Mohamed G.
, p. 3716 - 3724 (2017/11/21)
Based on the strategies of receptor structure-guided benzoxazinone design, a series of nitrogen nucleophiles such as benzyl amine, sodium azide, 4,4-bis o-toluidine, 4-butanolamine, glucosamine, 2-amino pyridine, 2-picolinyl amine, hydroxyl amine, and hydrazine derivatives, for example, hydrazine hydrate, semicarbazide, thiosemicarbazide, methylhydrazide, phenylhydrazide, could be reacted with 2-benzoxazine-2-yl benzoic acid 1. According the basicity of nucleophiles, regiospecific isomerization of benzoxazinone has been considered through formation of the spiro derivatives. Organic reagents can be controlled on the course of reaction of benzoxazinonyl benzoic acid 1. Preliminary bioassays indicated that the insecticidal spectra of the synthesized compounds were ecofriendly biodegradable materials due to isomerization. Among these analogues, the quinazoline 2–4 showed 100% mortality against Nilaparvata lugens (LC50?=?0.087?mg/L). The insecticidal potency of our designed analogues was dual-controlled by isomerization to quinazolinone and spiro derivatives that observed in vitro and shed light on the novel insecticidal mechanism. The chemical structure of the products can be confirmed by microanalytical, spectral data, optimized and stimulated by quantum chemical parameters.
Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors
Gilmore, John L.,Hays, Sheryl J.,Caprathe, Bradley W.,Lee, Chitase,Emmerling, Mark R.,Michael, Walter,Jaen, Juan C.
, p. 679 - 682 (2007/10/03)
A series of 2-aryl-4H-3,1-benzoxazin-4-ones have been synthesized and tested for inhibitory activity against C1r serine protease. Compounds were found that were equipotent and more selective than the reference compound FUT-175.
