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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
openaire +4 more sources
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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Dipyrimidine-based inhibitors of HIV-1 integrase
Expert Opinion on Investigational Drugs, 2003openaire +3 more sources