Results 271 to 280 of about 86,566 (299)

HIV INTEGRASE INHIBITORS

2022
HIV infection is incredibly detrimental and fatal to people. Unfortunately, despite recent advancements and medications, it has not yet been completely eradicated. Opportunistic infections are added to the list of disorders in AIDS (Acquired Immune Deficiency Syndrome), an infectious disease that develops as a result of an impaired immune system.
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HIV integrase inhibitors in ART-experienced patients

Current Opinion in HIV and AIDS, 2012
We 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 ...
Jose-Luis, Blanco, Javier, Martinez-Picado   +1 more
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Hydroxylated Aromatic Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1995
Efficient replication of HIV-1 requires integration of a DNA copy of the viral genome into a chromosome of the host cell. Integration is catalyzed by the viral integrase, and we have previously reported that phenolic moieties in compounds such as flavones, caffeic acid phenethyl ester (CAPE, 2), and curcumin confer inhibitory activity against HIV-1 ...
Terrence R. Jr. Burke, Mark Fesen, Abhijit Mazumder, Jessie Yung, Jian Wang, Adelaide M. Carothers, Dezider Grunberger, John Driscoll, Yves Pommier, Kurt Kohn   +9 more
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Benzyl amide-ketoacid inhibitors of HIV-integrase

Bioorganic & Medicinal Chemistry Letters, 2007
Integrase 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.
Michael A, Walker, Timothy, Johnson, B Narasimhulu, Naidu, Jacques, Banville, Roger, Remillard, Serge, Plamondon, Alain, Martel, Chen, Li, Albert, Torri, Himadri, Samanta, Zeyu, Lin, Ira, Dicker, Mark, Krystal, Nicholas A, Meanwell   +13 more
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Structure Based Drug Design: Clinically Relevant HIV-1 Integrase Inhibitors.

Current Topics in Medicinal Chemistry, 2019
HIV-1 integrase, a member of a polynucleotidyl transferases superfamily, catalyzes the insertion of the viral DNA into the genome of host cells. It has emerged as a potential target for developing anti-HIV agents.
Maninder Kaur, R. Rawal, Goutam Rath, A. Goyal   +3 more
semanticscholar   +1 more source

Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors

Bioorganic & Medicinal Chemistry Letters, 2007
A series of potent novel dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 6 is active against replication of HIV with a CIC(95) of 0.31 microM and exhibits no shift in potency in the presence of 50% normal human ...
John S, Wai, Boyoung, Kim, Thorsten E, Fisher, Linghang, Zhuang, Mark W, Embrey, Peter D, Williams, Donnette D, Staas, Chris, Culberson, Terry A, Lyle, Joseph P, Vacca, Daria J, Hazuda, Peter J, Felock, William A, Schleif, Lori J, Gabryelski, Lixia, Jin, I-Wu, Chen, Joan D, Ellis, Rama, Mallai, Steven D, Young   +18 more
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A new mechanism of resistance of HIV-2 to integrase inhibitors: a 5 amino-acids insertion in the integrase C-terminal domain.

Clinical Infectious Diseases, 2018
Background Integrase strand-transfer inhibitors (INSTI) are crucial for treatment of HIV-2 infection, due to limited available therapeutic options. Recently, bictegravir has been approved for HIV-1-infected patients but no data are currently available ...
Q. Le Hingrat, G. Collin, M. Lê, G. Peytavin, B. Visseaux, M. Bertine, R. Tubiana, M. Karmochkine, N. Valin, F. Collin, A. Lemaignen, L. Bernard, F. Damond, S. Matheron, D. Descamps, C. Charpentier   +15 more
semanticscholar   +1 more source

HIV Integrase Inhibitor Pharmacogenetics: An Exploratory Study

Clinical Drug Investigation, 2019
Integrase 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, David B. Cluck, Jonathan P. Moorman, Stacy D. Brown, Ke-Sheng Wang, Michelle M. Duffourc, Sam Harirforoosh   +6 more
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Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors

Bioorganic & Medicinal Chemistry, 2003
HIV-1 integrase (IN) is an essential enzyme for retroviral replication and a rational target for the design of anti-AIDS drugs. In the present study, we have designed, synthesized and tested a series of caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors.
Yu-Wen, Xu, Gui-Sen, Zhao, Cha-Gyun, Shin, Heng-Chang, Zang, Chong-Kyo, Lee, Yong Sup, Lee   +5 more
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HIV‐1 integrase inhibitors: 2005–2006 update

Medicinal Research Reviews, 2007
AbstractHIV‐1 integrase (IN) catalyzes the integration of proviral DNA into the host genome, an essential step for viral replication. Inhibition of IN catalytic activity provides an attractive strategy for antiretroviral drug design. Currently two IN inhibitors, MK‐0518 and GS‐9137, are in advanced stages of human clinical trials.
Raveendra, Dayam, Rambabu, Gundla, Laith Q, Al-Mawsawi, Nouri, Neamati   +3 more
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