Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors
In spite of significant progress in anti-HIV-1 therapy, current antiviral chemo-therapy still suffers from deleterious side effects and emerging drug resistance. Therefore, the development of novel antiviral drugs remains a crucial issue for the fight against AIDS. HIV-1 integrase is a key enzyme in...
| Main Authors: | , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2010-04-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/15/5/3048/ |
| _version_ | 1818859258764066816 |
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| author | Didier Desmaële Jean-François Mouscadet |
| author_facet | Didier Desmaële Jean-François Mouscadet |
| author_sort | Didier Desmaële |
| collection | DOAJ |
| description | In spite of significant progress in anti-HIV-1 therapy, current antiviral chemo-therapy still suffers from deleterious side effects and emerging drug resistance. Therefore, the development of novel antiviral drugs remains a crucial issue for the fight against AIDS. HIV-1 integrase is a key enzyme in the replication cycle of the retrovirus since it catalyzes the integration of the reverse transcribed viral DNA into the chromosomal DNA. Efforts to develop anti-integrase drugs started during the early nineties, culminating with the recent approval of Raltegravir. The discovery and the development of the styrylquinoline inhibitor class was an important step in the overall process. In this review we have described the key synthetic issues and the structure-activity relationship of this family of integrase inhibitors. Crystallographic and docking studies that shed light on their mechanism of action are also examined. |
| first_indexed | 2024-12-19T09:09:20Z |
| format | Article |
| id | doaj.art-d5f1d2ef090f467b991ff19ad48c6b7d |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-19T09:09:20Z |
| publishDate | 2010-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-d5f1d2ef090f467b991ff19ad48c6b7d2022-12-21T20:28:15ZengMDPI AGMolecules1420-30492010-04-011553048307810.3390/molecules15053048Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase InhibitorsDidier DesmaëleJean-François MouscadetIn spite of significant progress in anti-HIV-1 therapy, current antiviral chemo-therapy still suffers from deleterious side effects and emerging drug resistance. Therefore, the development of novel antiviral drugs remains a crucial issue for the fight against AIDS. HIV-1 integrase is a key enzyme in the replication cycle of the retrovirus since it catalyzes the integration of the reverse transcribed viral DNA into the chromosomal DNA. Efforts to develop anti-integrase drugs started during the early nineties, culminating with the recent approval of Raltegravir. The discovery and the development of the styrylquinoline inhibitor class was an important step in the overall process. In this review we have described the key synthetic issues and the structure-activity relationship of this family of integrase inhibitors. Crystallographic and docking studies that shed light on their mechanism of action are also examined.http://www.mdpi.com/1420-3049/15/5/3048/AIDSHIV-1integraseinhibitorstyrylquinoline |
| spellingShingle | Didier Desmaële Jean-François Mouscadet Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors Molecules AIDS HIV-1 integrase inhibitor styrylquinoline |
| title | Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors |
| title_full | Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors |
| title_fullStr | Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors |
| title_full_unstemmed | Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors |
| title_short | Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors |
| title_sort | chemistry and structure activity relationship of the styrylquinoline type hiv integrase inhibitors |
| topic | AIDS HIV-1 integrase inhibitor styrylquinoline |
| url | http://www.mdpi.com/1420-3049/15/5/3048/ |
| work_keys_str_mv | AT didierdesmaele chemistryandstructureactivityrelationshipofthestyrylquinolinetypehivintegraseinhibitors AT jeanfrancoismouscadet chemistryandstructureactivityrelationshipofthestyrylquinolinetypehivintegraseinhibitors |