Results 231 to 240 of about 28,079 (244)
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HIV integrase inhibitors in ART-experienced patients
Current Opinion in HIV and AIDS, 2012We review the most recent clinical trials of integrase inhibitors (INIs) in antiretroviral therapy (ART)-experienced patients, including trails of new strategies such as intensification and simplification therapy with this new class of compounds.After the excellent results of the first-generation INIs [raltegravir (RAL) and elvitegravir] in the ...
Javier Martinez-Picado, Jose-Luis Blanco
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Elvitegravir: An Emerging HIV Integrase Inhibitor
Future HIV Therapy, 2008Integration of the reverse transcribed HIV dsDNA into the host cell chromosome is critical for the subsequent production of progeny virions. In October 2007, the US FDA approved the first HIV-1 integrase inhibitor, raltegravir, as a therapeutic agent for treatment-experienced HIV-1-infected patients.
Eiichi Kodama, Kazuya Shimura
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Benzyl amide-ketoacid inhibitors of HIV-integrase
Bioorganic & Medicinal Chemistry Letters, 2007Integrase is one of three enzymes expressed by HIV and represents a validated target for therapy. Previous reports have demonstrated that the diketoacid-based chemotype is a useful starting point for the design of inhibitors of this enzyme. In this study, one of the ketone groups is replaced by a benzylamide resulting in a new potent chemotype.
Nicholas A. Meanwell +13 more
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HIV Integrase Inhibitor Pharmacogenetics: An Exploratory Study
Clinical Drug Investigation, 2019Integrase strand transfer inhibitors (INSTIs), dolutegravir, elvitegravir, and raltegravir, have become integral in the treatment of HIV, with close monitoring of continued efficacy and tolerability. As side effect occurrence varies among subjects receiving these drugs, we sought to perform an exploratory analysis examining the role of several single ...
Derek E. Murrell +6 more
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Catalytic Asymmetric Synthesis of an HIV Integrase Inhibitor
Organic Letters, 2008An efficient synthesis of HIV integrase inhibitor (S)-(-)-1 via a unique asymmetric hydrogenation of a mixture of imines/enamine 5a-5b/5c is described. Hydrogenation of the imines/enamine by a Rh(I)-Josiphos complex afforded 6 in 90% yield and 90% ee. Amide formation completed the synthesis of 1 in 58% overall yield from 2, which is readily available ...
Jaemoon Lee +6 more
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HIV-1 Resistance to Integrase Inhibitors
2017Over the past three decades, new antiretroviral drugs have been rapidly developed and expanded for use in the clinic. Antiretroviral therapy (ART) generally combines at least three different drugs for treatment of HIV-infected patients. As more new antiretroviral drugs (ARVs) belonging to different classes have become available, ART has greatly ...
Thibault Mesplède +2 more
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