Home HOME Acta Virologica 2012 Acta Virologica Vol.56, No.1, p.11-18, 2012

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ISSN 0001-723X
E-ISSN 1336-2305

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Acta Virologica Vol.56, No.1, p.11-18, 2012

Title: Evaluation of the in vitro antiretroviral potential of some Biginelli-type pyrimidines
Author: R. ZABIHOLLAHI, R. VAHABPOUR, C. HARTOONIAN, B. SEDAGHATI, S. M. SADAT, M. SOLEYMANI, M. RANJBAR, A. FASSIHI, M. R. AGHASADEGHI, H. R. MEMARIAN, M. SALEHI

Abstract: Despite the success of highly active antiretroviral therapy, AIDS still remains as one of the most important world health problems. Toxicity of current available drugs and inevitable emergence of multi-drug resistant strains makes things worse. In the present study a series of novel Biginelli-type pyrimidine compounds were evaluated as potential anti-human immunodeficiency virus (HIV)-1 agents using green fluorescence protein (GFP) reporter single round HIV-1 infection assay. The rate of infected cells was monitored by flowcytometry. The effect of compounds on the cellular proliferation was considered as the cyotoxicity. The anti-HIV-1 active compounds were selected for HIV-1 replication and syncytium formation assays. The antiretroviral activity of compounds was measured against luciferase reporter A murine leukemia virus (AMLV) virions as the retrovirus control. Compounds 2, 5, 6, 8, 11, 12, 13, 17, 18, 20, and 21 were the most potent against HIV-1. Compound 8 had the 50% inhibitory concentration (IC50) of 100 nmol/l for inhibiting HIV-1 replication and 50% cytotoxic concentration (CC50) was up to 100 μmol/l (therapeutic index (TI) >1000). Results show that the active compounds were able to inhibit the retrovirus control as well. Analysis of structure of the studied compounds proved relationships with their anti-HIV-1 effects. Some of the studied compounds seem to be promising anti-HIV-1 drug candidates. Structural manipulation based on the well-defined structure-activity relationships might propose some new leads for anti-HIV-1 drug discovery programs.

Keywords: antivirals; HIV-1; Biginelli-type pyrimidines
Year: 2012, Volume: 56, Issue: 1 Page From: 11, Page To: 18
doi:10.4149/av_2012_01_11
Price: 16.00 €






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