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Zahra Ghiasifar,Hafezeh Salehabadi,Neda Adibpour,Eskandar Alipour,Farzad Kobarfard,Mohammad Reza Shoushizadeh 대한화학회 2021 Bulletin of the Korean Chemical Society Vol.42 No.1
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??M compared with the azidothymidine as the reference drug (IC50 =?0.11??M). Results of the in vitro test and docking study were in good correlation.