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- W88668813 abstract "It is known that AIDS can nowadays be temporarily controlled, but not eradicated with current treatments against reverse transcriptase and protease. It is therefore important to identify new agents targeting HIV-1. Ln this respect, it is essential to develop inhibitors of the third essential enzyme of HIV-1 : integrase (IN). Our Laboratory bas recently reported that polyhydroxylated styrylquinolines are potent inhibitors of IN that block the replication of the virus in cell culture. In the present work, we report the preliminary results of our expanded SAR investigation directed towards the replacement of the ethylenic linker of the styrylquinolines by functionalized spacers: amide, hydrazide, urea or diketone-1,3 linker in order to increase affinity with the core domain of the protein. The results show that some of these new compounds have micromolar or submicromolar activities in the same range as styrylquinolines. However, an improvement of cytotoxicity is clearly noticed" @default.
- W88668813 created "2016-06-24" @default.
- W88668813 creator A5070678584 @default.
- W88668813 date "2003-01-01" @default.
- W88668813 modified "2023-09-24" @default.
- W88668813 title "Synthèse et activité biologique de nouveaux inhibiteurs de l'intégrase du VIH-1" @default.
- W88668813 hasPublicationYear "2003" @default.
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