Results 1 to 10 of about 3,561 (181)

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
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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
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[Resistance to integrase inhibitors].

Enfermedades infecciosas y microbiologia clinica, 2009
Integrase inhibitors are the most recently approved family of antiretroviral agents for the treatment of HIV infection. As with other antiretroviral agents, under pharmacological pressure, the virus selects resistance mutations if viral suppression is incomplete.
Carolina, Garrido, Carmen, de Mendoza, Vicente, Soriano   +2 more
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Primary resistance to integrase inhibitors in Shenzhen

Journal of Antimicrobial Chemotherapy, 2022
Abstract Objectives In recent years, integrase strand transfer inhibitor (INSTI)-containing regimens have been increasingly adopted in treatment for HIV/AIDS and promoted as non-occupational post-exposure prophylaxis in China.
Yue Zhu, Yuanmei Huang, Chenli Zheng, Jie Tang, Guang Zeng, Wei Xie, Hui Wang, Lukun Zhang, Shaochu Liu, Yan Zhang, Wei Tan, Jingguang Tan, Lijuan Jiang, Yun He, Liumei Xu, Zhengrong Yang, Jin Zhao   +16 more
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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
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Arylamide Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1997
Based 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.
H, Zhao, N, Neamati, A, Mazumder, S, Sunder, Y, Pommier, T R, Burke   +5 more
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The Hunt for HIV-1 Integrase Inhibitors

AIDS Patient Care and STDs, 2006
Currently, 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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Raltegravir: an integrase inhibitor for HIV-1

Expert Opinion on Investigational Drugs, 2008
The 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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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
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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
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