Results 171 to 180 of about 19,019 (189)
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Raltegravir: an integrase inhibitor for HIV-1
Expert Opinion on Investigational Drugs, 2008The need to develop antiretroviral agents with novel mechanisms of action persists for the treatment of both antiretroviral- experienced and antiretroviral-naive patients with HIV/AIDS. This is mandated, in part, by the perpetual advent of antiretroviral-resistant HIV-1 strains.
Martin Markowitz, Teresa H. Evering
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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.
Terrence R. Burke +8 more
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Arylamide Inhibitors of HIV-1 Integrase
Journal of Medicinal Chemistry, 1997Based on data derived from a large number of HIV-1 integrase inhibitors, similar structural features can be observed, which consist of two aryl units separated by a central linker. For many inhibitors fitting this pattern, at least one aryl ring also requires ortho bis-hydroxylation for significant inhibitory potency.
Abhijit Mazumder +5 more
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The future of integrase inhibitors of HIV-1
Current Opinion in Virology, 2012Integration of the HIV-1 DNA is required and essential to maintain the viral DNA in the infected cell. Integration process occurs in several events, mainly endonucleolytic processing of the 3' ends of the viral DNA and strand transfer or joining of the viral and cellular DNA.
Anne-Geneviève Marcelin +2 more
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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
Yves Pommier, Nouri Neamati
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Development of Integrase Inhibitors for Treatment of AIDS: An Overview.
ChemInform, 2007AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Harshita Lavania +2 more
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Quinoline-based HIV Integrase Inhibitors
Current Pharmaceutical Design, 2013HIV integrase became an important target for drug development more than twenty years ago. However, progress has been hampered by the lack of assays suitable for high throughput screening, a reliable crystal structure or pharmacophore. Thus, a real breakthrough was only observed in 2007 with the introduction of the first integrase inhibitor, raltegravir,
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Journal of the American Academy of Physician Assistants, 2016
Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral agents used to treat HIV. These drugs--raltegravir, elvitegravir, and dolutegravir--are preferred options for treatment-naïve patients when used in combination with two nucleoside reverse transcriptase inhibitors.
Nathan Trustman +2 more
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Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral agents used to treat HIV. These drugs--raltegravir, elvitegravir, and dolutegravir--are preferred options for treatment-naïve patients when used in combination with two nucleoside reverse transcriptase inhibitors.
Nathan Trustman +2 more
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Hydrazide-Containing Inhibitors of HIV-1 Integrase
Journal of Medicinal Chemistry, 1997Inhibitors of HIV integrase are currently being sought as potential new therapeutics for the treatment of AIDS. A large number of inhibitors discovered to date contain the o-bis-hydroxy catechol structure. In an effort to discover structural leads for the development of new HIV integrase inhibitors which do not rely on this potentially cytotoxic ...
George W. A. Milne +7 more
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