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[Resistance to integrase inhibitors].
Enfermedades infecciosas y microbiologia clinica, 2009Integrase inhibitors are the most recently approved family of antiretroviral agents for the treatment of HIV infection. As with other antiretroviral agents, under pharmacological pressure, the virus selects resistance mutations if viral suppression is incomplete.
Carolina, Garrido +2 more
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The clinical pharmacology of integrase inhibitors
Expert Review of Clinical Pharmacology, 2018Introduction: Treatment of HIV infection has consistently evolved in the last three decades. A steady improvement in efficacy tolerability, safety, and practical aspects of treatment intake has made HIV infection much easier to manage over the long term, and in optimal treatment conditions the life expectancy of persons living with HIV infection now ...
Di Perri, Giovanni +3 more
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Coumarin-Based Inhibitors of HIV Integrase
Journal of Medicinal Chemistry, 1997The structures of a large number of HIV-1 integrase inhibitors have in common two aryl units separated by a central linker. Frequently at least one of these aryl moieties must contain 1,2-dihydroxy substituents in order to exhibit high inhibitory potency.
H, Zhao +8 more
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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 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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Thiazolothiazepine Inhibitors of HIV-1 Integrase
Journal of Medicinal Chemistry, 1999A series of thiazolothiazepines were prepared and tested against purified human immunodeficiency virus type-1 integrase (HIV-1 IN) and viral replication. Structure-activity studies reveal that the compounds possessing the pentatomic moiety SC(O)CNC(O) with two carbonyl groups are in general more potent against purified IN than those containing only one
NEAMATI N. +12 more
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Next-Generation Integrase Inhibitors
Drugs, 2013The integrase enzyme facilitates the incorporation of HIV-1 proviral DNA into the host cell genome and catalyses a function vital to viral replication. Inhibitors of this enzyme represent the newest class of antiretroviral drugs in our armamentarium to treat HIV-1 infection.
Sharon L, Karmon, Martin, Markowitz
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Inhibitors of Human Immunodeficiency Virus Integrase
1999Integration of the viral DNA into a host cell chromosome is an essential step for HIV replication and maintenance of persistent infection. Two viral factors are essential for integration: the viral DNA termini (the att sites) and IN. Accruing knowledge of the IN structure, catalytic mechanisms, and interactions with other proteins can be used to design
Y, Pommier, N, Neamati
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Integrase inhibitor gains FDA approval
American Journal of Health-System Pharmacy, 2007Merck on October 12 announced the approval of raltegravir, an HIV integrase inhibitor, as part of a combination regimen in treatment-experienced HIV-infected adults whose virus is active and resistant to multiple antiviral agents.
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[Integrase inhibitor, CCR5 antagonist, fusion inhibitor].
Nihon rinsho. Japanese journal of clinical medicine, 2010Integrase inhibitors have a novel antiretroviral mechanism which prevents proviral DNA integration into the CD4+ cell chromosome. Promising results have been seen in clinical trials in treatment-naïve and -experienced infected individuals. CCR5 antagonists bind to CCR5, one of the second receptors of HIV-1, and inhibit HIV-1 entry into CD4+ cells ...
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