Results 231 to 240 of about 30,099 (284)

Integrase inhibitors to treat HIV/Aids

Nature Reviews Drug Discovery, 2005
HIV integrase is a rational target for treating HIV infection and preventing AIDS. It took approximately 12 years to develop clinically usable inhibitors of integrase, and Phase I clinical trials of integrase inhibitors have just begun. This review focuses on the molecular basis and rationale for developing integrase inhibitors.
Yves, Pommier, Allison A, Johnson, Christophe, Marchand   +2 more
openaire   +4 more sources

Novel integrase inhibitors for HIV

Expert Opinion on Investigational Drugs, 2010
Integrase inhibitors are the newest class of antiretroviral agents developed to treat HIV-1 infection. Raltegravir (RAL), the only integrase inhibitor (INI) currently approved for the treatment of HIV-infected patients, has proven to be a potent and well-tolerated antiretroviral (ARV) agent.
Nicole, Prada, Martin, Markowitz
openaire   +2 more sources

Potential Inhibitors of HIV Integrase

Nucleosides and Nucleotides, 1999
In the search for inhibitors of HIV integrase, the enzyme involved in the integration of viral DNA into host DNA, we have synthesized and studied a number of analogs of the heterocyclic molecule, chloroquine.
C, Mathé, V, Nair
openaire   +2 more sources

Tolerability of HIV integrase inhibitors

Current Opinion in HIV and AIDS, 2012
This review discusses the available safety data for three integrase strand transfer inhibitors (INSTIs)--raltegravir, elvitegravir and dolutegravir--derived from studies in both HIV-infected and HIV-uninfected cohorts.Phase 2 and 3 clinical trials show that all three INSTIs are well tolerated in treatment-naive and treatment-experienced patients with ...
Frederick J, Lee, Andrew, Carr
openaire   +2 more sources

Resistance to HIV integrase inhibitors

Current Opinion in HIV and AIDS, 2012
HIV integrase inhibitors are potent antiretroviral drugs that efficiently decrease viral load in patients. Emergence of resistance mutations against this new class of drugs represents a threat to their long-term efficacy. The purpose of this review is to provide new information about the most recent mutations identified and other mutations that confer ...
Thibault, Mesplède, Peter K, Quashie, Mark A, Wainberg   +2 more
openaire   +2 more sources

Coumarin-Based Inhibitors of HIV Integrase

Journal of Medicinal Chemistry, 1997
The 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, N, Neamati, H, Hong, A, Mazumder, S, Wang, S, Sunder, G W, Milne, Y, Pommier, T R, Burke   +8 more
openaire   +2 more sources

Raltegravir: The first HIV integrase inhibitor

Clinical Therapeutics, 2008
The availability of new classes of antiretroviral drugs has made it possible for HIV-infected individuals who are highly treatment experienced to achieve the goals of immunologic recovery and virologic suppression. Raltegravir is the first integrase inhibitor to be approved by the US Food and Drug Administration for use in antiretroviral treatment ...
Jennifer, Cocohoba, Betty J, Dong
openaire   +2 more sources

Thiazolothiazepine Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1999
A 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., TURPIN J. A, WINSLOW H. E., CHRISTENSEN J. L., WILLIAMSON K., ORR A., RICE W. G., POMMIER Y., GAROFALO A., BRIZZI A., CAMPIANI G., FIORINI I., NACCI V.   +12 more
openaire   +4 more sources