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• W2108333435 abstract "5′-O-(4-fluorosulphonylbenzoyl)-esters of ribavirin (FSBR), adenosine (FSBA), guanosine (FSBG) and inosine (FSBI) were obtained by acylation of the 5′-OH of adenosine, guanosine, inosine, and ribavirin with 4-fluorosulphonylbenzoyl chloride (FSBCl) in HMPA. The above derivatives were tested as inhibitors of nucleoside triphosphatase (NTPase)/helicase activities of Flaviviridae: hepatitis C virus (HCV), West Nile virus (WNV), Japanese encephalitis virus (JEV) and dengue virus (DENV) and polymerase activity of HCV and WNV. When the unwinding activity of viral NTPase/helicases was tested under standard conditions, only weak inhibition was obtained with FSBI (IC 50 ≥120 μM) and in the case of FSBG even an activation was seen. The preincubation of the NTPase/helicases with the 5′-O-FSB derivatives increased the inhibitory effect. Screening of the 5′-O-FSB derivatives on inhibition of the WNV and HCV RNA polymerases employing GTP or UTP substrates revealed rather modest inhibitory effect. FSBI exhibited the highest inhibitory activity against WNV (IC 50 =70 μM with UTP substrate) and HCV polymerase (IC 50 =80 μM with GTP substrate). Other 5′-O-FSB derivatives were very weak inhibitors or completely failed to show any activity against HCV and WNV enzymes. In contrast to the NTPase/helicases the preincubation of the polymerases did not influence the inhibition." @default.
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• W2108333435 date "2004-02-01" @default.
• W2108333435 modified "2023-09-23" @default.
• W2108333435 title "Synthesis and Evaluation of ATP-Binding Site Directed Potential Inhibitors of Nucleoside Triphosphatases/ Helicases and Polymerases of Hepatitis C and other Selected <i>Flaviviridae</i> Viruses" @default.
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• W2108333435 doi "https://doi.org/10.1177/095632020401500104" @default.
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