Synthesis and antiviral activity of new thiazole, 1,2,4-triazol and oxindole derivatives
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RADUL, Oleg; SUCMAN, Natalia; POGREBNOI, Serghei; BARBĂ, Alic; MACAEV, Fliur. Synthesis and antiviral activity of new thiazole, 1,2,4-triazol and oxindole derivatives . In: Chemistry Journal of Moldova. 2011, nr. 1(6), pp. 101-109. ISSN 1857-1727.
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Chemistry Journal of Moldova
Numărul 1(6) / 2011 / ISSN 1857-1727 /ISSNe 2345-1688

Synthesis and antiviral activity of new thiazole, 1,2,4-triazol and oxindole derivatives

Pag. 101-109

Radul Oleg, Sucman Natalia, Pogrebnoi Serghei, Barbă Alic, Macaev Fliur
 
Institutul de Chimie al AŞM
 
Disponibil în IBN: 29 noiembrie 2013


Rezumat

The synthesis and antiviral activity evaluation of new derivatives of 2-aminothiazole, 1,2,4-triazole, as well as oxindoles has been realized. The synthesized compounds exhibited different cytotoxicity, in particular, oxindols 4 , 5 , 7 , 8 , 9, 10, 11, 12, 13, 58 as well as thiazole/triazole 73 and 75 turned out to be the most cytotoxic for MT-4 cell lines. The compounds 11, 12, 73, and 75 are more toxic than reference compound Efavirenz. As far as the antiviral activity is concerned, none of the title compounds turned out active against Reo-1, Sb-1, VSV, RSV, YFV and VV viruses. The results obtained against Bovine Viral Diarrhoea Virus (BVDV) showed that nine compounds (six from oxindol’s seria 6, 12, 13, 52, 56, 58 and three 73, 75, 77 of triazole homologues) resulted moderate active. Among all of them, the most potent compound was 52, with EC50 of 6.6 μM. Studies of effect of synthesized compounds against Coxsakie Virus (CVB-2) revealed that only two compounds, 13 and 73 exhibit moderate activity (EC50 >40 and >18 μM, respectively). It should be noticed that eleven compounds, 4, 5, 7, 8, 9, 10, 11, 12, 13, 58, and 75 showed moderate activity against HIV-1 (EC50 >16 – m >59μM).

Cuvinte-cheie
2-aminothiazole, 4-triazol, oxindoles,

1, 2