Synthesis and evaluation of hexahydropyrimidines and diamines as novel hepatitis C virus inhibitors SCIE SCOPUS

Cited 18 time in WEB OF SCIENCE Cited 0 time in Scopus
Title
Synthesis and evaluation of hexahydropyrimidines and diamines as novel hepatitis C virus inhibitors
Author(s)
Hwang, Jong Yeon; Kim, Hee-Young; Jo, Suyeon; Park, Eunjung; Choi, Jihyun; Kong, Sunju; Park, Dong-Sik; Heo, Ja Myung; Lee, Jong Seok; Ko, Yoonae; Choi, Inhee; Cechetto, Jonathan; Kim, Jaeseung; Lee, Jinhwa; No, Zaesung; Windisch, Marc Peter
KIOST Author(s)
Lee, Jong Seok(이종석)
Alternative Author(s)
이종석
Publication Year
2013-12
Abstract
In order to identify novel anti-hepatitis C virus (HCV) agents we devised cell-based strategies and screened phenotypically small molecule chemical libraries with infectious HCV particles, and identified a hit compound (1) containing a hexahydropyrimidine (HHP) core. During our cell-based SAR study, we observed a conversion of HHP 1 into a linear diamine (6), which is the active component in inhibiting HCV and exhibited comparable antiviral activity to the cyclic HHP I. In addition, we engaged into the biological characterization of HHP and demonstrated that HHP does not interfere with HCV RNA replication, but with entry and release of viral particles. Here we report the results of the preliminary SAR and mechanism of action studies with HHP. (C) 2013 Elsevier Masson SAS. All rights reserved.
ISSN
0223-5234
URI
https://sciwatch.kiost.ac.kr/handle/2020.kiost/3047
DOI
10.1016/j.ejmech.2013.09.055
Bibliographic Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.70, pp.315 - 325, 2013
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Subject
DERIVATIVES; DISCOVERY
Keywords
Hepatitis C virus; Phenotypic screening; Hexahydropyrimidine; Diamines; Entry; Release
Type
Article
Language
English
Document Type
Article
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
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