Results 251 to 260 of about 71,892 (273)
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Practical Synthesis of a HIV Integrase Inhibitor
Organic Process Research & Development, 2008A practical and efficient synthesis of the potent HIV integrase inhibitor 1 is described. Starting from readily available 3,4-dihydro-2H-pyran, the six-step synthesis features a through process without purification of any of the intermediates until the isolation of crystalline intermediate 7.
David A. Conlon +14 more
openaire +2 more sources
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 ...
Javier Martinez-Picado, Jose-Luis Blanco
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Structure Based Drug Design: Clinically Relevant HIV-1 Integrase Inhibitors.
Current Topics in Medicinal Chemistry, 2019HIV-1 integrase, a member of a polynucleotidyl transferases superfamily, catalyzes the insertion of the viral DNA into the genome of host cells. It has emerged as a potential target for developing anti-HIV agents.
Maninder Kaur +3 more
semanticscholar +1 more source
HIV integrase inhibitors as therapeutic agents in AIDS
Reviews in Medical Virology, 2007AbstractHIV‐1 integrase is a protein of Mr 32 000 encoded at the 3′‐end of the pol gene. Integration of HIV DNA into the host cell chromosomal DNA apparently occurs by a carefully defined sequence of DNA tailoring (3′‐processing (3′P)) and coupling (integration) reactions.
Vasu Nair, Guochen Chi
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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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Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity
Iranian journal of pharmaceutical research, 2016HIV-1 integrase (IN) enzyme, one of the three main enzymes of HIV-1, catalyzed the insertion of the viral DNA into the genome of host cells. Because of the lack of its homologue in human cells and its essential role in HIV-1 replication, IN inhibition ...
Z. Hajimahdi, A. Zarghi
semanticscholar +1 more source
Elvitegravir: An Emerging HIV Integrase Inhibitor
Future HIV Therapy, 2008Integration of the reverse transcribed HIV dsDNA into the host cell chromosome is critical for the subsequent production of progeny virions. In October 2007, the US FDA approved the first HIV-1 integrase inhibitor, raltegravir, as a therapeutic agent for treatment-experienced HIV-1-infected patients.
Eiichi Kodama, Kazuya Shimura
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Journal of Medicinal Chemistry, 2019
A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on HIV-1 integrase, an attractive target for antiviral chemotherapy, was prepared and screened for ...
K. Peese +20 more
semanticscholar +1 more source
A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on HIV-1 integrase, an attractive target for antiviral chemotherapy, was prepared and screened for ...
K. Peese +20 more
semanticscholar +1 more source
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.
Nicholas A. Meanwell +13 more
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Quinoline, Coumarin and Other Heterocyclic Analogs Based HIV-1 Integrase Inhibitors.
Current Drug Discovery Technologies, 2017Human Immunodeficiency Virus Type 1 Integrase or HIV-1 integrase (IN) is a 288 amino acid protein that incorporates the retrotranscribed viral DNA into the host chromosomal DNA.
P. Wadhwa +3 more
semanticscholar +1 more source