58006-91-0Relevant academic research and scientific papers
Synthesis of Biuret Derivatives as Potential HIV-1 Protease Inhibitors Using (LDHs-g-HMDI-Citric Acid), as a Green Recyclable Catalyst
Ghiasifar, Zahra,Salehabadi, Hafezeh,Adibpour, Neda,Alipour, Eskandar,Kobarfard, Farzad,Shoushizadeh, Mohammad Reza
, p. 48 - 59 (2020/12/07)
In this study, a novel catalyst based on layered double hydroxides (LDHs) attached by hexamethylene-1,6-diisocyanate (HMDI) and citric acid (LDHs-g-HMDI-Citric acid) is reported and used to increase the yield of biurets synthesis. Biuret derivatives 5a–n were prepared by reaction of several phenyl allophanates (3a–d), which prepared from the reaction of phenyl chloroformate and urea derivatives (2a–d), with variously substituted amines (4a–g) in the presence of LDHs-g-HMDI-Citric acid as a reusable heterogeneous catalyst at reflux condition for 60–180 min. These biurets (5a–n) were evaluated for human immunodeficiency virus type-1 (HIV-1) protease inhibitory activity by HIV-1 p24 antigen ELISA kit and six of them (5n, 5i, 5j, 5 m, 5f, and 5a) showed moderate activity on HIV-1 virus with IC50 values ranging from 55 to 100 μM compared with the azidothymidine as the reference drug (IC50 = 0.11 μM). Results of the in vitro test and docking study were in good correlation.
Synthesis and cytotoxicity of some biurets against human breast cancer T47D cell line
Fouladdel, Shamileh,Khalaj, Ali,Adibpour, Neda,Azizi, Ebrahim
supporting information; scheme or table, p. 5772 - 5775 (2010/11/24)
Design, synthesis and cytotoxicity of several known and novel biurets against human breast cancer T47D cell line in comparison to doxorubicin are described. Biurets incorporating 2-methyl quinoline-4-yl and benzo[d]thiazol-2-ylthio moieties showed higher cytotoxicity and decreased cell viability in a concentration- and time-dependent manner.
Nouvelles syntheses de phenyl-4 allophanates
Al Sabbagh, Mohamed Mowafak,Calmon, Michelle,Calmon, Jean-Pierre
, p. 73 - 77 (2007/10/02)
The synthesis of eighteen alkyl or phenyl 4-phenylallophanates is described.The classical methods used for the preparation of allophanates - namely, condensation between an isocyanate and a carbamate, reaction between a urea and a carbonate, desulphurization of 3-thioallophanic acid esters - proved to be unsuitable for the synthesis of 4-phenylallophanic acid phenyl esters.Variously substituted 4-phenylallophanates can be obtained by reacting a chloroformate with a phenylurea in the presence of pyridine, which promotes the transfer of the carboxylate group.The occurence of electrondonating substituents, such as CH3, at the nitrogen atom receiving the carboxylate group promotes the reaction.The low yields observed for aliphatic esters can be accounted for by the instability of the alkyl chloroformate-pyridine complex.The structures of the derivatives synthesized was corroborated by the analysis of their n.m.r. and u.v. spectra. Non-commercial phenyl chloroformates were prepared by reacting phosgene with a sodium phenolate in the presence of anhydrous benzene.
Process for preparing 2,4-dihaloquinazolines
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, (2008/06/13)
A one-step process for the preparation of 2,4-dihaloquinazolines is disclosed beginning with methoxycarbonyl- or phenoxycarbonyl-derivatives of substituted phenylureas which are cyclized and concomitantly halogenated with a cyclizing-halogenating reagent such as N,N-dimethylaniline in phosphorus oxychloride. The 2,4-dihaloquinazolines of the instant process are particularly valuable as intermediates in the preparation of 4-amino-2-(4-substituted-piperazin-1-yl) quinazolines useful in the treatment of cardiovascular disorders such as hypertension.
