4,552 publications from this institution
Abstract Das Cyanid (I) addiert Benzylmercaptan zur Verbindung (II), die über den Thioether (IV) in die im Titel genannte Verbindung (V) umgewandelt wird.
A series of silicon-containing polyoxotungstates belonging to the ‘Keggin-type’ (‘Keggin’, ‘Keggin sandwich’) were evaluated for their antiviral activity against enveloped viruses (myxo-, herpes- and retroviruses). The compounds exhibited antiviral activity against influenza virus type A, respiratory syncytial virus (RSV), herpes simplex virus type-1 (HSV-1), type-2 (HSV-2), thymidine kinase-deficient (TIC) HSV-1, human cytomegalovirus (HCMV), human immunodeficiency virus type-1 (HIV-1) and type-2 (HIV-2) at concentrations that were well below their cytotoxic threshold. The ‘Keggin’ compound JM2815 (K 5 [Si-(TiCp)W 11 O 39 ].12H 2 O) and the ‘Keggin sandwich’ compound JM1590 (K 13 [Ce(SiW 11 O 39 ) 2 ].26H 2 O) resulted in the highest selectivity indices against HIV-1 and HIV-2, and compound JM2820 ([Me 3 NH] 8 .[Si 2 Nb 6 W 18 O 77 ]) was the most potent inhibitor of HSV and HCMV replication. These compounds proved active against HCMV and HSV when present during virus adsorption, and against influenza virus A and RSV when present after virus adsorption. Polyoxosilicotungstates inhibited the binding of radiolabeled HCMV particles to the cells at concentrations that were antivirally active, and the compounds were able to displace HCMV particles that were bound to a heparin-Sepharose matrix. Presumably, the polyoxosilicotungstates interact with positively charged domains on the viral envelope site(s) involved in the attachment of the (HCMV) virions to the cell surface receptor heparan sulphate.
This work analyses the effects of electrical conductivities of dielectric and cobalt amount on output parameters such as metal removal rate and the surface roughness value of cemented carbides cut by wire electrical discharge machining(W-EDM). Especially, the cracking behaviour of W-EDM machined surface and optimal machining condition of three kinds of cemented carbides, which have different chemical composition of tungsten carbide and cobalt are also tested. Experimental result shows that increases in cobalt content and electrical conductivity of the dielectric affect the metal removal rate and substantially worsen the final surface quality as a greater quantity of solidified metal deposits on the eroded surface.
No abstract is provided for this article.
Abstract Two series of fluoroacyclic nucleosides were synthesised by condensation of nucleic acid bases with substituted fluoropentanes. 1-(5′-Fluoro-4′-hydroxypentyl)-cytosine showed a modest activity against cytomegalovirus (MIC50: 12–15 μg/ml). All the other compounds were inactive against all the viruses tested.
National audience
Virtually all the compounds that are currently used (or have been the subject of advanced clinical trials) for the treatment of HIV infections, belong to one of the following classes: (i) nucleoside reverse transcriptase inhibitors (NRTIs): i.e., zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir, emtricitabine and nucleotide reverse transcriptase inhibitors (NtRTIs) (i.e., tenofovir disoproxil fumarate); (ii) non-nucleoside reverse transcriptase inhibitors (NNRTIs): i.e., nevirapine, delavirdine, efavirenz, emivirine; and (iii) protease inhibitors (PIs): i.e., saquinavir, ritonavir, indinavir, nelfinavir, amprenavir and lopinavir. In addition to the reverse transcriptase and protease reaction, various other events in the HIV replicative cycle can be considered as potential targets for chemotherapeutic intervention: (i) viral adsorption, through binding to the viral envelope glycoprotein gp120 (polysulfates, polysulfonates, polycarboxylates, polyoxometalates, polynucleotides, and negatively charged albumins); (ii) viral entry, through blockade of the viral coreceptors CXCR4 (i.e., bicyclam (AMD3100) derivatives) and CCR5 (i.e., TAK-779 derivatives); (iii) virus-cell fusion, through binding to the viral envelope glycoprotein gp41 (T-20, T-1249); (iv) viral assembly and disassembly, through NCp7 zinc finger-targeted agents (2,2′-dithiobisbenzamides (DIBAs), azadicarbonamide (ADA)); (v) proviral DNA integration, through integrase inhibitors such as 4-aryl-2,4-dioxobutanoic acid derivatives; (vi) viral mRNA transcription, through inhibitors of the transcription (transactivation) process (flavopiridol, fluoroquinolones). Also, various new NRTIs, NNRTIs and PIs have been developed that possess, respectively: (i) improved metabolic characteristics (i.e., phosphoramidate and cyclosaligenyl pronucleotides by-passing the first phosphorylation step of the NRTIs), (ii) increased activity (“second” generation NNRTIs (i.e., TMC-125, DPC-083)) against those HIV strains that are resistant to the “first” generation NNRTIs, or (iii), as in the case of PIs, a different, modified peptidic (i.e., azapeptidic (atazanavir)) or non-peptidic scaffold (i.e., cyclic urea (mozenavir), 4-hydroxy-2-pyrone (tipranavir)). Non-peptidic PIs may be expected to inhibit HIV mutant strains that have become resistant to peptidomimetic PIs.
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.