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language of document : English
Material Type : طرح تحقیقاتی/ پروژه لاتین
Record number : 51494
doc. No : R3140
main entry : Zabihollahi, Rezvan
title & author : Evaluation of the in vitro antiretroviral potential of some biginelli - type pyrimidines [Research Project]/Executer: Rezvan Zabihollahi, Mansour Salehi; ETC: Mohammad Memarian, Afshin Fasihi, Mohammad Reza Agha Sadeghi, Rahele Namazi, Farhang Vahabpour, Mehdi Sadat
Publication statement : Isfahan: Isfahan University of Medical Sciences, Vice Chancellery for Research , 2011.
Physical Description : Various Paging.:tab
Notes : عنوان به فارسی : بررسی توان ضد‭ HIV‬تعداد‭ ۱۰ ‬مشتق جدید‭ ۳ ‬و‭ ۴ ‬دی ه‌یدروپریمیدین -‭ ۲‬- اون
Notes : 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 ?mol/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.
Notes : Print
descriptor : Anti-Retroviral Agents
: Acquired Immunodeficiency Syndrome
: Pyrimidines
Originating Source : IRIsfahan University of Medical Sciences
publication type : p
Source : Vice Chancellery for Research
Ended Date : 2011
Project code : 185155
 
 
 
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