Results 221 to 230 of about 118,861 (266)
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Enamino-oxindole HIV protease inhibitors
Bioorganic and Medicinal Chemistry Letters, 2012We have designed and synthesized a series of HIV protease inhibitors (PIs) with enamino-oxindole substituents optimized to interact with the S2' subsite of the HIV protease binding pocket. Several of these inhibitors have sub-nanomolar K(i) and antiviral IC(50) in the low nM range against WT HIV and against a panel of multi-drug resistant (MDR) strains.
Michael, Eissenstat +8 more
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Resistance to HIV protease inhibitors
Haemophilia, 1998Summary. Resistance to the HIV‐1 protease inhibitor indinavir involves the accumulation of multiple amino acid substitutions in the viral protease. A minimum of 11 amino acid positions have been identified as potential contributors to phenotypic resistance.
C. A. Lee +5 more
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Heterocyclic HIV-Protease Inhibitors
Current Medicinal Chemistry, 2013In the panorama of HIV protease inhibitors (HIV PIs), many efforts have been devoted to the development of new compounds with reduced peptidic nature in order to improve pharmacokinetics and pharmacodynamics features. The introduction of cyclic scaffolds in the design of new chemical entities reduces flexibility and affords more rigid inhibitors ...
CALUGI, CHIARA +2 more
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Hyperlipidemia and inhibitors of HIV protease
Current Opinion in Clinical Nutrition and Metabolic Care, 2001HIV protease inhibitors have been successfully incorporated into therapy for patients with HIV. These otherwise efficacious treatments present with multiple metabolic side-effects and body habitus changes known as the lipodystrophy syndrome. Direct associations of the lipid abnormalities with protease inhibitor use have been described, and ongoing ...
O, Distler +3 more
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Prodrugs of HIV Protease Inhibitors
Current Pharmaceutical Design, 2003Despite the efficiency of the present polytherapies against AIDS, HIV replication continues indicating difficulties in drug adherence, drug-drug interactions, resistance issues, and the existence of reservoirs or sanctuaries for the virus. Moreover, most of the current FDA-approved HIV protease inhibitors (PIs) display disadvantageous physicochemical ...
Pierre, Vierling, Jacques, Greiner
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Peptidomimetic Inhibitors of HIV Protease
Current Topics in Medicinal Chemistry, 2004There are currently (July, 2002) six protease inhibitors approved for the treatment of HIV infection, each of which can be classified as peptidomimetic in structure. These agents, when used in combination with other antiretroviral agents, produce a sustained decrease in viral load, often to levels below the limits of quantifiable detection, and a ...
John T, Randolph, David A, DeGoey
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Journal of Enzyme Inhibition, 1992
The human immunodeficiency virus (HIV), the etiological agent for the acquired immune deficiency syndrome (AIDS), is a retrovirus which makes use of a virally-encoded aspartic protease to perform specific proteolytic processing of two of its gene products in order to form active enzymes and structural proteins within the mature virion.
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The human immunodeficiency virus (HIV), the etiological agent for the acquired immune deficiency syndrome (AIDS), is a retrovirus which makes use of a virally-encoded aspartic protease to perform specific proteolytic processing of two of its gene products in order to form active enzymes and structural proteins within the mature virion.
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Perspectives in HIV Protease Inhibitors
1996The therapy of HIV-1, the causative agent of AIDS, is limited today to a small number of different drugs, all of which are nucleoside analogues. Nucleoside analogues active against HIV are all inhibitors of reverse transcriptase (RT) and target primarily early events in the replication cycle of HIV.
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Drug Interactions of HIV Protease Inhibitors
Drug Safety, 1999All the currently available protease inhibitors are metabolised by the cytochrome P450 (CYP) enzyme system. All are inhibitors of CYP3A4, ranging from weak inhibition for saquinavir to very potent inhibition for ritonavir. Thus, they are predicted to have numerous drug interactions, although few such interactions have actually been documented either in
L I, Malaty, J J, Kuper
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HIV-1 protease inhibitors in development
Expert Opinion on Investigational Drugs, 2002Several pharmaceutical companies have developed an increasing number of second generation protease inhibitors (PI) during the last few years. Many of these compounds have been in preclinical trials and some are now in clinical use. All drugs in this category have been designed to be well absorbed and overcome the crucial problem of cross-resistance ...
S. Rusconi, S. La Seta Catamancio
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