Expert Opinion on Therapeutic Patents · 2002 · 78 citations · 26 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryMolecular VirologyAntiretroviral TherapyAntiviral AgentsAntiviral PharmacologyAntiviral TherapyLigand BindingNatural Product-based Drug DesignAntiviral Drug DesignHiv Antiretroviral TherapyIntegrase ProteinsIntegrase Strand Transfer InhibitorsPhase Ii Clinical TrialsSmall Molecule Drug DesignTherapeutic Target IdentificationViral Entry Inhibitors
AbstractValidation of integrase as a suitable therapeutic target for the development of drugs against HIV infection; discovery of diketo acid derivatives as bona fide inhibitors of integrase and the recent news of Phase II clinical trials with S-1360 are major findings fuelling the recent surge of interest in the development of integrase inhibitors. Herein, the first review of the entire patent literature for small molecule intergrase inhibitors is presented. The emphasis is based on compounds with potential to serve as leads, therefore, no attempts are made to include: antibodies, oligonucleotides or polypeptides.Keywordsdiketoacidsdrug discoveryHIV-1 integraseinhibitor designnatural productsS-1360
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Inhibitors of human immunodeficiency virus integrase.
Mark R. Fesen, Kurt W. Kohn, François Leteurtre et al. · Proceedings of the National Academy of Sciences · 1993 · 279 citations · Full text