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The different classes of HIV integrase inhibitors Volume 11, supplement 3, Numéro spécial : L’intégrase du VIH et ses inhibiteurs

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Laboratoire de chimie organique et macromoléculaire associé au CNRS, Université des Sciences et Technologies de Lille, 59655 Villeneuve d’Ascq

Since the discovery of the first integrase inhibitors in 1993, it takes about seven years to synthesize the first strand transfer inhibitors and presumably about the same time to the launch of the first antiviral agents targeting this enzyme. In this paper we describe the two main families of integrase inhibitors : the polyphenols, non specific integrase inhibitors and diketoacids and derivatives, strand transfer inhibitors. Some non specific integrase inhibitors targeting other steps of the replicative cycle of the virus were isolated from natural sources (mainly from the vegetable kingdom), whereas the pharmaceutical research yield the discovery of selective integrase antivirals. The structural prerequisites allowing the synthesis of good integrase inhibitors able to block the viral replication are described as well as the mutations associated with integrase inhibitor resistance. The presumed mechanism of action of these inhibitors in the active site of the enzyme is given.