Author: Hwang, Nicky; Ban, Haiqun; Chen, Junjun; Ma, Julia; Liu, Hui; Lam, Patrick; Kulp, John; Menne, Stephan; Chang, Jinhong; Guo, Ju-Tao; Du, Yanming
Title: Synthesis of 4-oxotetrahydropyrimidine-1(2H)-carboxamides derivatives as capsid assembly modulators of hepatitis B virus Cord-id: z36yyqth Document date: 2021_1_11
ID: z36yyqth
Snippet: We report herein the synthesis and evaluation of phenyl ureas derived from 4-oxotetrahydropyrimidine as novel capsid assembly modulators of hepatitis B virus (HBV). Among the derivatives, compound 27 (58031) and several analogs showed an activity of submicromolar EC(50) against HBV and low cytotoxicities (>50 μM). Structure–activity relationship studies revealed a tolerance for an additional group at position 5 of 4-oxotetrahydropyrimidine. The mechanism study indicates that compound 27 (5803
Document: We report herein the synthesis and evaluation of phenyl ureas derived from 4-oxotetrahydropyrimidine as novel capsid assembly modulators of hepatitis B virus (HBV). Among the derivatives, compound 27 (58031) and several analogs showed an activity of submicromolar EC(50) against HBV and low cytotoxicities (>50 μM). Structure–activity relationship studies revealed a tolerance for an additional group at position 5 of 4-oxotetrahydropyrimidine. The mechanism study indicates that compound 27 (58031) is a type II core protein allosteric modulator (CpAMs), which induces core protein dimers to assemble empty capsids with fast electrophoresis mobility in native agarose gel. These compounds may thus serve as leads for future developments of novel antivirals against HBV.
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