Development of Integrase Inhibitors of Quinolone Acid Derivatives for Treatment of AIDS: An Overview

Z.      G. Luo; J.      J. Tan; Y.      Zeng; C.      X. Wang; L.      M. Hu

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