Abstract
HIV-1 integrase (IN), which has no cellular counterpart, has been intensely studied over the past 15 years and has been fully validated as a therapeutic target with the first FDA approved IN inhibitor raltegravir. The quinolone acid GS-9137 (elvitegravir), which most probably will become the next candidate of IN inhibitors, is in the process of enrolling patients in the phase III clinical trials. This review focuses on small-molecular of quinolone acid derivatives, which have the similar pharmacophore of β-diketoacids, as integrase inhibitors with antiviral activity.
Keywords: Drug discovery, diketoacides, HIV-1, inhibitors, integrase, quinolone acid derivatives, Integrase Inhibitors, Quinolone Acid, AIDS, HIV-1 integrase (IN), GS-9137, HIV-1, inhibitors, HIV-1 replication process, Transcriptase inhibitors (NRTIs), Co-receptor inhibitor (CRI), Virus-drug resistance, Antiretroviral therapy (HAART), Catalytic core domain (CCD), Inhibit viral integration of diketo-acid derivatives, NADPH-dependent, 3D-QSAR, Structure-activity relationship (SAR), Anti-IN activity, Inhibitory potency, Current antiviral drugs, Fusion inhibitor, Half maximal inhibitory concentration, Reverse transcriptase
Mini-Reviews in Medicinal Chemistry
Title: Development of Integrase Inhibitors of Quinolone Acid Derivatives for Treatment of AIDS: An Overview
Volume: 10 Issue: 11
Author(s): Z. G. Luo, J. J. Tan, Y. Zeng, C. X. Wang and L. M. Hu
Affiliation:
Keywords: Drug discovery, diketoacides, HIV-1, inhibitors, integrase, quinolone acid derivatives, Integrase Inhibitors, Quinolone Acid, AIDS, HIV-1 integrase (IN), GS-9137, HIV-1, inhibitors, HIV-1 replication process, Transcriptase inhibitors (NRTIs), Co-receptor inhibitor (CRI), Virus-drug resistance, Antiretroviral therapy (HAART), Catalytic core domain (CCD), Inhibit viral integration of diketo-acid derivatives, NADPH-dependent, 3D-QSAR, Structure-activity relationship (SAR), Anti-IN activity, Inhibitory potency, Current antiviral drugs, Fusion inhibitor, Half maximal inhibitory concentration, Reverse transcriptase
Abstract: HIV-1 integrase (IN), which has no cellular counterpart, has been intensely studied over the past 15 years and has been fully validated as a therapeutic target with the first FDA approved IN inhibitor raltegravir. The quinolone acid GS-9137 (elvitegravir), which most probably will become the next candidate of IN inhibitors, is in the process of enrolling patients in the phase III clinical trials. This review focuses on small-molecular of quinolone acid derivatives, which have the similar pharmacophore of β-diketoacids, as integrase inhibitors with antiviral activity.
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Cite this article as:
G. Luo Z., J. Tan J., Zeng Y., X. Wang C. and M. Hu L., Development of Integrase Inhibitors of Quinolone Acid Derivatives for Treatment of AIDS: An Overview, Mini-Reviews in Medicinal Chemistry 2010; 10 (11) . https://dx.doi.org/10.2174/1389557511009011046
DOI https://dx.doi.org/10.2174/1389557511009011046 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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