SYNTHESIS AND ANTIVIRAL ACTIVITY OF NEW THIAZOLE, 1,2,4-TRIAZOL AND OXINDOLE DERIVATIVES
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 a...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Academy of Sciences of Moldova, Institute of Chemistry
2011-06-01
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| Series: | Chemistry Journal of Moldova: General, Industrial and Ecological Chemistry |
| Subjects: | |
| Online Access: | http://www.cjm.asm.md/sites/default/files/article_files/Macaev%20101-109.pdf |
| Summary: | 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). |
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| ISSN: | 1857-1727 2345-1688 |