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Characterization of Antiviral Activity of Benzamide Derivative AH0109 against HIV-1 Infection
Author(s) -
Liyu Chen,
Zhujun Ao,
Kallesh D. Jayappa,
Gary Kobinger,
ShuiPing Liu,
Guojun Wu,
Mark A. Wainberg,
Xiaojian Yao
Publication year - 2013
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.00100-13
Subject(s) - lamivudine , virology , reverse transcriptase , raltegravir , zidovudine , nevirapine , biology , human immunodeficiency virus (hiv) , viral replication , drug , benzamide , viral disease , pharmacology , virus , chemistry , viral load , rna , biochemistry , stereochemistry , hepatitis b virus , gene , antiretroviral therapy
In the absence of an effective vaccine against HIV-1 infection, anti-HIV-1 strategies play a major role in disease control. However, the rapid emergence of drug resistance against all currently used anti-HIV-1 molecules necessitates the development of new antiviral molecules and/or strategies against HIV-1 infection. In this study, we have identified a benzamide derivative named AH0109 that exhibits potent anti-HIV-1 activity at an 50% effective concentration of 0.7 μM in HIV-1-susceptible CD4+ C8166 T cells. Mechanistic analysis revealed that AH0109 significantly inhibits both HIV-1 reverse transcription and viral cDNA nuclear import. Furthermore, our infection experiments indicated that AH0109 is capable of disrupting the replication of HIV-1 strains that are resistant to the routinely used anti-HIV-1 drugs zidovudine, lamivudine, nevirapine, and raltegravir. Together, these findings provide evidence for a newly identified antiviral molecule that can potentially be developed as an anti-HIV-1 agent.

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