In view of the selective anti-HSV activity of 1,5-anhydro-2,3-dideoxy-2- (5-iodouracil-1-yl)-D-arabino-hexitol, a series of novel 1,5-anhydrohexitol nucleosides were synthesized and evaluated for their inhibitory activity against several viruses. The 5-iodouracil 3 and the 5-ethyluracil 4 derivatives are highly selective TK-dependent inhibitors of HSV-1 and HSV-2. Broad anti-herpes virus activity was noticed for 5-fluorocytosine 6 and 2,6-diaminopurine 10 analogues. From a transport study of 3, using the thymidine influx competition method, one can conclude that intracellular uptake of this compound most probably occurs by passive diffusion. X-ray analysis of compounds 3 and 9 showed that the heterocyclic base of 1,5-anhydrohexitol pyrimidine and purine is placed in the axial position and that the sugar ring adopts a slightly distorted chair conformation.
2'-Deoxyuridines with a five-membered heterocyclic substituent in the 5-position were synthesized by palladium-catalyzed coupling reactions of 5-iodo-2'-deoxyuridine with the activated heteroaromatics. Further modification of the compound with the 5-thien-2-yl substituent gave 5-(5-bromothien-2-yl)-2'-deoxyuridine and 5-(5-chlorothienyl-2-yl)-2'-deoxyuridine. Both compounds show potent and selective activity against herpes simplex virus type 1 and varicella-zoster virus.
Chlorite-oxidized oxypolysaccharides are polyacetal carboxylic acids. They inhibited the cytopathic effect of vesicular stomatitis virus in mouse embryo cell cultures challenged at low input multiplicity. After intraperitoneal injection of these compounds in mice, interferon appeared in the circulation. The compounds also protected mice against lethal mengovirus infection and against the development of experimental pox lesions on the tail. Chlorite-oxidized oxyamylose was antiviral only when at least 64% of the glucopyranose units were oxidized, an observation which suggested a correlation between charge density and antiviral effect. The antiviral activity was also influenced by the molecular weight, as demonstrated by the fact that chlorite-oxidized dextrans which had a high intrinsic viscosity were more active than those with low intrinsic viscosity. ' "Bevoegdverklaard navorser" of the Belgian N.F.W.O. 2 "Aangesteld navorser" of the Belgian N.F.W.O.
The solubility of CO 2 in the molten ternary eutectic mixture with literature data but the solubility value reported in this work is much higher than most of those reported in the Li 2 CO 3 -Na 2 CO 3 -K 2 CO 3 (43.5, 31.5, 25.0 mol.%) at 973 K has been determined by a titration technique. From the obtained literature. A chemical dissolution of CO 2 as C 2 O 5 2is proposed and the consequences of the occurrence of this titration curve, the solubility has been found to amount to 9.5·10 -2 mol·L -1 (σ = 1.0) under a pressure of CO 2 of 1 atm species on the acidobasic properties of molten carbonates are discussed. It appears from the experimental results that the and the pK d value of the carbonate melt has been evaluated to 5.37 (σ 5 = 0.24) if the concentrations of the solutes are CO 2 /C 2 O 5 2equilibrium in the carbonate melt is a slow process. expressed in mol·L -1 . This pK d value is in good agreementThe scales described in this way are quite satisfactory Fax: (internat.) ϩ32-10/472330
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