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...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2015-09-01
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| Series: | Acta Pharmaceutica Sinica B |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211383515001057 |
| _version_ | 1811283591314800640 |
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| author | Changyuan Wang Zhendong Song Haiqing Yu Kexin Liu Xiaodong Ma |
| author_facet | Changyuan Wang Zhendong Song Haiqing Yu Kexin Liu Xiaodong Ma |
| author_sort | Changyuan Wang |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-04-13T02:14:19Z |
| format | Article |
| id | doaj.art-ed51cec71eba4151970ff030f4146b6f |
| institution | Directory Open Access Journal |
| issn | 2211-3835 2211-3843 |
| language | English |
| last_indexed | 2024-04-13T02:14:19Z |
| publishDate | 2015-09-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Acta Pharmaceutica Sinica B |
| spelling | doaj.art-ed51cec71eba4151970ff030f4146b6f2022-12-22T03:07:12ZengElsevierActa Pharmaceutica Sinica B2211-38352211-38432015-09-015543144110.1016/j.apsb.2015.07.002Adenine: an important drug scaffold for the design of antiviral agentsChangyuan WangZhendong SongHaiqing YuKexin LiuXiaodong MaAdenine 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.http://www.sciencedirect.com/science/article/pii/S2211383515001057AntiviralStructure–activity relationshipAdenineAcyclic nucleoside phosphonatesScaffold |
| spellingShingle | Changyuan Wang Zhendong Song Haiqing Yu Kexin Liu Xiaodong Ma Adenine: an important drug scaffold for the design of antiviral agents Acta Pharmaceutica Sinica B Antiviral Structure–activity relationship Adenine Acyclic nucleoside phosphonates Scaffold |
| 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 | Antiviral Structure–activity relationship Adenine Acyclic nucleoside phosphonates Scaffold |
| url | http://www.sciencedirect.com/science/article/pii/S2211383515001057 |
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