Results 241 to 250 of about 30,099 (284)
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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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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 ...
H, Zhao +7 more
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The Hunt for HIV-1 Integrase Inhibitors
AIDS Patient Care and STDs, 2006Currently, there are three distinct mechanistic classes of antiretrovirals: inhibitors of the HIV- 1 reverse transcriptase and protease enzymes and inhibitors of HIV entry, including receptor and coreceptor binding and cell fusion. A new drug class that inhibits the HIV-1 integrase enzyme (IN) is in development and may soon be available in the clinic ...
Max, Lataillade, Michael J, Kozal
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Integrase Inhibitors Against HIV: Efficacy and Resistance
Future Virology, 2016Divisione Clinicizzata di Malattie Infettive, Dipartimento di Scienze Biomediche e Cliniche ‘Luigi Sacco’, Universita degli Studi di Milano, via G.B. Grassi 74, 20157 Milano, Italy *Author for correspondence: Tel.: +39 02 5031 9761; Fax: +39 02 5031 9758; stefano.rusconi@unimi ...
P. Tau, S. Rusconi
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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.
Teresa H, Evering, Martin, Markowitz
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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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HIV integrase inhibitors in ART-experienced patients
Current Opinion in HIV and AIDS, 2012We 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 +1 more
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Hydroxylated Aromatic Inhibitors of HIV-1 Integrase
Journal of Medicinal Chemistry, 1995Efficient 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 +9 more
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Benzyl amide-ketoacid inhibitors of HIV-integrase
Bioorganic & Medicinal Chemistry Letters, 2007Integrase 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 +13 more
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Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors
Bioorganic & Medicinal Chemistry Letters, 2007A 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 +18 more
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