Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.

Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.

By using a fragment-assembly strategy and bioisosteric-replacement principle, a series of novel piperazine derivatives were designed, synthesized, and evaluated for their cellular target-effector fusion activities and in vitro antiviral activities against HIV-1. Preliminary structure-activity relati...

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Main Authors: Tao Liu, Zhiyong Weng, Xiaowu Dong, Linjie Chen, Ling Ma, Shan Cen, Naiming Zhou, Yongzhou Hu
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2013-01-01
Series:PLoS ONE
Online Access:http://europepmc.org/articles/PMC3538727?pdf=render
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spelling doaj-c3e8ba9dd709452fa6d407370557e3792020-11-25T02:15:21ZengPublic Library of Science (PLoS)PLoS ONE1932-62032013-01-0181e5363610.1371/journal.pone.0053636Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.Tao LiuZhiyong WengXiaowu DongLinjie ChenLing MaShan CenNaiming ZhouYongzhou HuBy using a fragment-assembly strategy and bioisosteric-replacement principle, a series of novel piperazine derivatives were designed, synthesized, and evaluated for their cellular target-effector fusion activities and in vitro antiviral activities against HIV-1. Preliminary structure-activity relationships (SARs) of target compounds were concluded in this study, and five compounds were found to exhibited medium to potent CCR5 fusion activities with IC(50) values in low micromolar level. Among evaluated compounds, 23 h was found to be a CCR5 antagonist with an IC(50) value of 6.29 µM and an anti-HIV-1 inhibitor with an IC(50) value of 0.44 µM.http://europepmc.org/articles/PMC3538727?pdf=render
collection DOAJ
language English
format Article
sources DOAJ
author Tao Liu
Zhiyong Weng
Xiaowu Dong
Linjie Chen
Ling Ma
Shan Cen
Naiming Zhou
Yongzhou Hu
spellingShingle Tao Liu
Zhiyong Weng
Xiaowu Dong
Linjie Chen
Ling Ma
Shan Cen
Naiming Zhou
Yongzhou Hu
Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.
PLoS ONE
author_facet Tao Liu
Zhiyong Weng
Xiaowu Dong
Linjie Chen
Ling Ma
Shan Cen
Naiming Zhou
Yongzhou Hu
author_sort Tao Liu
title Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.
title_short Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.
title_full Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.
title_fullStr Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.
title_full_unstemmed Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.
title_sort design, synthesis and biological evaluation of novel piperazine derivatives as ccr5 antagonists.
publisher Public Library of Science (PLoS)
series PLoS ONE
issn 1932-6203
publishDate 2013-01-01
description By using a fragment-assembly strategy and bioisosteric-replacement principle, a series of novel piperazine derivatives were designed, synthesized, and evaluated for their cellular target-effector fusion activities and in vitro antiviral activities against HIV-1. Preliminary structure-activity relationships (SARs) of target compounds were concluded in this study, and five compounds were found to exhibited medium to potent CCR5 fusion activities with IC(50) values in low micromolar level. Among evaluated compounds, 23 h was found to be a CCR5 antagonist with an IC(50) value of 6.29 µM and an anti-HIV-1 inhibitor with an IC(50) value of 0.44 µM.
url http://europepmc.org/articles/PMC3538727?pdf=render
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AT lingma designsynthesisandbiologicalevaluationofnovelpiperazinederivativesasccr5antagonists
AT shancen designsynthesisandbiologicalevaluationofnovelpiperazinederivativesasccr5antagonists
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