Synthesis, characterization and antiviral evaluation of 1,3-Thiazolidine-4-one derivatives bearing L-Valine side chain

Year 2012, Volume: 16 Issue: 3, 181 - 193, 07.03.2014

Esra Tatar İlkay Küçükgüzel Erik De Clercq Ramalingam Krishnan Neerja Basu

Abstract

ABSTRACT: 1,3-Thiazolidine-4-ones have been known to possess anti-HIV and anti-HCV activity
as they are, respectively, HIV-1 non-nucleoside reverse transcriptase inhibitors and HCV
NS5B RNA-dependent RNA-polymerase inhibitors. Some novel 1-[2-(benzoylamino)-
3-methylbutyryl]-4-alkyl/arylalkylthiosemicarbazides, 2-[2-(benzoylamino)-3-methylbutyrylhydrazono]-
3-alkyl-/arylalkyl- 5-non substituted/methyl-1,3-thiazolidinones, were synthesized
and evaluated for their antiviral activity. Antiviral activity of the synthesized compounds were
screened against various types of viruses (Feline Corona Virus (FIPV), Feline Herpes Virus,
HSV-1(KOS), HSV-1(TK-KOS ACVr), HSV-2(G), Vaccinia virus, Vesicular stomatitis virus, Varicella-
ZosterVirus TK+VZV, Varicella-ZosterVirus TK-VZV, Cytomegalovirus, Respiratory syncytial virus,
Coxsackie B4 virus, Parainfluenza-3 virus, Reovirus-1, Sindbis virus and Punta Toro virus) in
CRFK, HEL, HeLa and Vero cell cultures. Anti-HIV and cytotoxicity data were also obtained
with the compounds using the strains HIV-1 (IIIB) and HIV-2 (ROD) in an MT-4/MTT based assay.
None of the tested compounds showed antiviral activity at subtoxic concentrations. For
all the synthesized compounds anti-HCV NS5B RdRp activity was not observed at the concentration
of 100 μM which was the highest concentration tested.
KEYWORDS: 4-Thiazolidinones, L-valine, anti-HIV activity, anti-HCV activity.

Keywords

4-Thiazolidinones, L-valine, anti-HIV activity, anti-HCV activity

Synthesis, characterization and antiviral evaluation of 1,3-Thiazolidine-4-one derivatives bearing L-Valine side chain

Abstract

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