Summary. -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 immunodefi ciency virus (HIV)-1 agents using green fl uorescence protein (GFP) reporter single round HIV-1 infection assay. Th e rate of infected cells was monitored by fl owcytometry. Th e eff ect of compounds on the cellular proliferation was considered as the cyotoxicity. Th e anti-HIV-1 active compounds were selected for HIV-1 replication and syncytium formation assays. Th e 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 (IC 50 ) of 100 nmol/l for inhibiting HIV-1 replication and 50% cytotoxic concentration (CC 50 ) 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 eff ects. Some of the studied compounds seem to be promising anti-HIV-1 drug candidates. Structural manipulation based on the well-defi ned structure-activity relationships might propose some new leads for anti-HIV-1 drug discovery programs.Keywords: antivirals; HIV-1; Biginelli-type pyrimidines * Co-corresponding authors. E-mail: fassihi@pharm.mui.ac.ir, mrasadeghi@pasteur.ac.ir; phone: +98-311-7922562, +98-21 66468765.Abbreviations: AMLV = A murine leukemia virus; DHPMs = 3,4-dihydropyrimidine-2(1H)-ones; ENV(s) = envelope glycoprotein(s); GFP = green fl uorescence protein; HAART = highly active antiretroviral therapy; HIV = human immunodefi ciency virus; IN = integrase; RT = reverse transcriptase; RTU = reverse transcriptase unit; SCR = single-cycle replicable; IC 50 = 50% inhibitory concentration; CC 50 = 50% cytotoxic concentration; SI = selectivity index (CC 25 / IC 25 ); TI = therapeutic index (CC 50 /IC 50 ); VSVG = vesicular stomatitis virus-glycoprotein

An ADA reaction between AD-2 and FU-3 was theoretically studied within two uncatalyzed as well as catalyzed pathways.

In the present work, the V 2 O 5 /S-doped graphitic carbon nitride nanocomposite was constructed using the in-situ growth method. The properties of this interesting material were improved by S-doping as well as addition of V 2 O 5 . The nanocomposite was characterized using FT-IR, XRD, SEM, EDX, BET, TEM, PL, XPS and UV-DRS techniques. In continuation, the constructed nanocomposite was applied for adsorption and degradation of methylene blue and phenol as organic pollutants. The effect of certain factors such as pH, doses of adsorbent and adsorbate (methylene blue and phenol), time, and temperature was evaluated through performing of adsorption under different conditions. Then, degradation of the pollutants was performed under various conditions such as sunlight, light-emitting diode, and ultraviolet irradiations and also in dark. The results showed a significant increase in the adsorption and photocatalytic activities of V 2 O 5 /S-doped graphitic carbon nitride in comparison with pristine graphitic carbon nitride. The performance of V 2 O 5 /S-doped graphitic carbon nitride remained after treatment for five times.

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