Results 231 to 240 of about 42,534 (266)
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Patented HIV-1 Integrase Inhibitors (1998-2005)
Recent Patents on Anti-Infective Drug Discovery, 2006Combination therapy, comprising at least three anti-human immunodeficiency virus (anti-HIV) drugs, has become the standard treatment of AIDS. Since 1996, highly active antiretroviral therapy (HAART) was designed to rapidly control HIV replication. It has had a significant impact on patient health and progression of AIDS in developed countries but its ...
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HIV‐1 Integrase Inhibitors: Update and Perspectives
2008Publisher Summary The chapter focuses on the recent advances in understanding the cellular mechanisms of human immunodeficiency virus (HIV) integration and the sites of actions of inhibitors. The chapter presents list of the known mutations that have been characterized for HIV‐1 integrase (IN) with their impact on IN activity, viral replication, and ...
Elena A, Semenova +2 more
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Chicoric Acid Analogues as HIV-1 Integrase Inhibitors
Journal of Medicinal Chemistry, 1999The present study was undertaken to examine structural features of L-chicoric acid (3) which are important for potency against purified HIV-1 integrase and for reported cytoprotective effects in cell-based systems. Through a progressive series of analogues, it was shown that enantiomeric D-chicoric acid (4) retains inhibitory potency against purified ...
Z, Lin +14 more
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Novel furocoumarins as potential HIV-1 integrase inhibitors
Bioorganic Chemistry, 2014A series of seven novel, rationally designed N-substituted 3-{3,5-dimethylfuro[3,2-g]coumarin-6-yl}propanamides have been prepared as potential HIV-1 integrase (IN) inhibitors via a five-step pathway commencing with resorcinol and diethyl 2-acetylglutarate, and the HIV-1 IN inhibition potential of these compounds has been examined relative to ...
Temitope O. Olomola +6 more
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Substituted 2-pyrrolinone inhibitors of HIV-1 integrase
Bioorganic & Medicinal Chemistry Letters, 2007The beta-diketoacid class of HIV-1 integrase (IN) inhibitors represent the first potent class of compounds specific for the strand transfer catalytic activity of the viral enzyme. Previously, utilizing a beta-diketoacid pharmacophore as a search query, we identified a substituted 2-pyrrolinone with modest IN inhibitory activity from a database of small-
Raveendra, Dayam +2 more
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Molecular modelling of HIV-1 integrase
2021The author retains copyright of this thesis. It must only be used for personal non-commercial research, education and study. It must not be used for any other purposes and may not be transmitted or shared with others without prior permission. For further terms on this licence: https://rightsstatements.org/page/InC-EDU/1.0/?language=en Contact ...
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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 ...
Ying-Shan Han +2 more
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HIV-1 Integrase Strand Transfer Inhibitors
2010Publisher Summary This chapter focuses on a new class of antiretroviral agents called “integrase (IN) strand transfer inhibitors” that exert their pharmacological effect by preventing the incorporation of viral DNA into host chromatin. The evolution of HIV-1IN strand transfer inhibitors has been one of the most significant advances in the field of ...
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Structure and function of retroviral integrase
Nature Reviews Microbiology, 2021Goedele N Maertens +2 more
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