685505-75-3Relevant academic research and scientific papers
Discovery of potent antiviral (HSV-1) quinazolinones and initial structure-activity relationship studies
Brown, Carla E.,Kong, Tiffany,McNulty, James,D'Aiuto, Leonardo,Williamson, Kelly,McClain, Lora,Piazza, Paolo,Nimgaonkar, Vishwajit L.
, p. 4601 - 4605 (2017)
The discovery of antiviral activity of 2,3-disubstituted quinazolinones, prepared by a one-pot, three-component condensation of isatoic anhydride with amines and aldehydes, against Herpes Simplex Virus (HSV)-1 is reported. Sequential iterative synthesis/a
Larvicidal activities of 2-aryl-2,3-dihydroquinazolin -4-ones against malaria vector anopheles arabiensis, in silico ADMET prediction and molecular target investigation
Abed, Sara Nidal,Akrawi, Sabah H.,Aldhubiab, Bandar E.,Alwassil, Osama I.,Attimarad, Mahesh,Bataineh, Yazan A.,Bhandary, Subhrajyoti,Chandrashekharappa, Sandeep,Chopra, Deepak,Deb, Pran Kishore,Girish, Meravanige B.,Gleiser, Raquel M.,Haroun, Michelyne,Khalil, Hany Ezzat,Mohanlall, Viresh,Morsy, Mohamed A.,Nair, Anroop B.,Palenge, Ramachandra,Pottathil, Shinu,Ramachandra, Pushpalatha,Sreeharsha, Nagaraja,Tratrat, Christophe,Venugopala, Katharigatta N.,Venugopala, Rashmi
, (2020/03/19)
Malaria, affecting all continents, remains one of the life-threatening diseases introduced by parasites that are transmitted to humans through the bites of infected Anopheles mosquitoes. Although insecticides are currently used to reduce malaria transmission, their safety concern for living systems, as well as the environment, is a growing problem. Therefore, the discovery of novel, less toxic, and environmentally safe molecules to effectively combat the control of these vectors is in high demand. In order to identify new potential larvicidal agents, a series of 2-aryl-1,2-dihydroquinazolin-4-one derivatives were synthesized and evaluated for their larvicidal activity against Anopheles arabiensis. The in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of the compounds were also investigated and most of the derivatives possessed a favorable ADMET profile. Computational modeling studies of the title compounds demonstrated a favorable binding interaction against the acetylcholinesterase enzyme molecular target. Thus, 2-aryl-1,2-dihydroquinazolin-4-ones were identified as a novel class of Anopheles arabiensis insecticides which can be used as lead molecules for the further development of more potent and safer larvicidal agents for treating malaria.
Method for synthesis of quinazolinone derivative
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Paragraph 0092-0095, (2017/04/20)
The invention discloses a method for synthesis of quinazolinone; the method comprises the steps of starting from o-aminobenzamide, taking water as a solvent, carrying out a ring-enlargement reaction with benzaldehyde, to generate a dihydroquinazolinone intermediate, and then under participation of a metal iridium complex, dehydrogenating to obtain the quinazolinone derivative; the reaction shows three remarkable advantages: 1) the reaction is carried out in an aqueous solution so as to reduce use of a large amount of organic solvents, and water is a cheap, green and safe solvent; 2) the reaction avoids use of highly toxic oxidants, so as to avoid damage to the environment; and 3) hydrogen gas generated from the reaction is a by-product, and has no environmental pollution; therefore, the reaction accords with the requirements of green chemistry, and has broad prospects for development.
Base mediated synthesis of 2-aryl-2,3-dihydroquinazolin-4(1H)-ones from 2-aminobenzonitriles and aromatic aldehydes in water
Wu, Xiao-Feng,Oschatz, Stefan,Block, Axel,Spannenberg, Anke,Langer, Peter
supporting information, p. 1865 - 1870 (2014/03/21)
An environmentally friendly and mild procedure to obtain 2,3-dihydroquinazolin-4(1H)-ones from 2-aminobenzonitriles and aromatic aldehydes has been developed. The reactions took place in water with inorganic base (K3PO4) as the only promoter. Various desired products have been prepared in moderate to good yields under identical conditions. Further transformation of dihydroquinazolinones to quinazolinones was carried out as well with TBHP as the oxidant.
