Cargando…

Adenine: an important drug scaffold for the design of antiviral agents

Adenine derivatives, in particular the scaffold bearing the acyclic nucleoside phosphonates (ANPS), possess significant antiviral and cytostatic activity. Till now, several effective adenine derivatives have been marketed for the treatment of HIV, HBV, CMV and other virus-infected diseases. These co...

Descripción completa

Detalles Bibliográficos
Autores principales: Wang, Changyuan, Song, Zhendong, Yu, Haiqing, Liu, Kexin, Ma, Xiaodong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4629444/
https://www.ncbi.nlm.nih.gov/pubmed/26579473
http://dx.doi.org/10.1016/j.apsb.2015.07.002
_version_ 1782398578150342656
author Wang, Changyuan
Song, Zhendong
Yu, Haiqing
Liu, Kexin
Ma, Xiaodong
author_facet Wang, Changyuan
Song, Zhendong
Yu, Haiqing
Liu, Kexin
Ma, Xiaodong
author_sort Wang, Changyuan
collection PubMed
description Adenine derivatives, in particular the scaffold bearing the acyclic nucleoside phosphonates (ANPS), possess significant antiviral and cytostatic activity. Till now, several effective adenine derivatives have been marketed for the treatment of HIV, HBV, CMV and other virus-infected diseases. These compounds are represented by tenofovir (PMPA), a medicine for both HIV and HBV, and adefovir as an anti-HBV agent. More than this, other analogs, such as GS9148, GS9131, and GS7340, are also well-known anti-viral agents that have been progressed to the clinical studies for their excellent activity. In general, the structures of these compounds include an adenine nucleobase linked to a phosphonate side chain. Considerable structural modifications on the scaffold itself and the peripheral sections were made. The structure-activity relationships (SARs) of this skeleton will provide valuable clues to identify more effective adenine derivatives as antiviral drugs. Here, we systematically summarized the SARs of the adenine derivatives, and gave important information for further optimizing this template.
format Online
Article
Text
id pubmed-4629444
institution National Center for Biotechnology Information
language English
publishDate 2015
publisher Elsevier
record_format MEDLINE/PubMed
spelling pubmed-46294442015-11-17 Adenine: an important drug scaffold for the design of antiviral agents Wang, Changyuan Song, Zhendong Yu, Haiqing Liu, Kexin Ma, Xiaodong Acta Pharm Sin B Review Adenine derivatives, in particular the scaffold bearing the acyclic nucleoside phosphonates (ANPS), possess significant antiviral and cytostatic activity. Till now, several effective adenine derivatives have been marketed for the treatment of HIV, HBV, CMV and other virus-infected diseases. These compounds are represented by tenofovir (PMPA), a medicine for both HIV and HBV, and adefovir as an anti-HBV agent. More than this, other analogs, such as GS9148, GS9131, and GS7340, are also well-known anti-viral agents that have been progressed to the clinical studies for their excellent activity. In general, the structures of these compounds include an adenine nucleobase linked to a phosphonate side chain. Considerable structural modifications on the scaffold itself and the peripheral sections were made. The structure-activity relationships (SARs) of this skeleton will provide valuable clues to identify more effective adenine derivatives as antiviral drugs. Here, we systematically summarized the SARs of the adenine derivatives, and gave important information for further optimizing this template. Elsevier 2015-09 2015-09-02 /pmc/articles/PMC4629444/ /pubmed/26579473 http://dx.doi.org/10.1016/j.apsb.2015.07.002 Text en © 2015 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Review
Wang, Changyuan
Song, Zhendong
Yu, Haiqing
Liu, Kexin
Ma, Xiaodong
Adenine: an important drug scaffold for the design of antiviral agents
title Adenine: an important drug scaffold for the design of antiviral agents
title_full Adenine: an important drug scaffold for the design of antiviral agents
title_fullStr Adenine: an important drug scaffold for the design of antiviral agents
title_full_unstemmed Adenine: an important drug scaffold for the design of antiviral agents
title_short Adenine: an important drug scaffold for the design of antiviral agents
title_sort adenine: an important drug scaffold for the design of antiviral agents
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4629444/
https://www.ncbi.nlm.nih.gov/pubmed/26579473
http://dx.doi.org/10.1016/j.apsb.2015.07.002
work_keys_str_mv AT wangchangyuan adenineanimportantdrugscaffoldforthedesignofantiviralagents
AT songzhendong adenineanimportantdrugscaffoldforthedesignofantiviralagents
AT yuhaiqing adenineanimportantdrugscaffoldforthedesignofantiviralagents
AT liukexin adenineanimportantdrugscaffoldforthedesignofantiviralagents
AT maxiaodong adenineanimportantdrugscaffoldforthedesignofantiviralagents