Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines.
Several 4-substituted 1,3,5-triazino[1,2-a]benzimidazol-2-amines were prepared via cyclization of 2-benzimidazolylguanidine with various reactants. The prototropic tautomerism in the obtained dihydro analogs was investigated. According to the NMR data, the 3,4-dihydro form was found to predominate i...
| Main Authors: | , |
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| Format: | Journal Article |
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Springer
2007
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| Online Access: | http://hdl.handle.net/20.500.11937/16544 |
| _version_ | 1848749206585475072 |
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| author | Dolzhenko, Anton Chui, W. |
| author_facet | Dolzhenko, Anton Chui, W. |
| author_sort | Dolzhenko, Anton |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | Several 4-substituted 1,3,5-triazino[1,2-a]benzimidazol-2-amines were prepared via cyclization of 2-benzimidazolylguanidine with various reactants. The prototropic tautomerism in the obtained dihydro analogs was investigated. According to the NMR data, the 3,4-dihydro form was found to predominate in DMSO solutions. All tested compounds inhibited the activity of mammalian dihydrofolate reductase. The most active compound was 4,4-dimethyl-3,4-dihydro[1,3,5]triazino[1,2-a]benzimidazol-2-amine (IC50 = 10.9 microM). |
| first_indexed | 2025-11-14T07:17:15Z |
| format | Journal Article |
| id | curtin-20.500.11937-16544 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T07:17:15Z |
| publishDate | 2007 |
| publisher | Springer |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-165442017-09-13T15:42:22Z Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines. Dolzhenko, Anton Chui, W. Several 4-substituted 1,3,5-triazino[1,2-a]benzimidazol-2-amines were prepared via cyclization of 2-benzimidazolylguanidine with various reactants. The prototropic tautomerism in the obtained dihydro analogs was investigated. According to the NMR data, the 3,4-dihydro form was found to predominate in DMSO solutions. All tested compounds inhibited the activity of mammalian dihydrofolate reductase. The most active compound was 4,4-dimethyl-3,4-dihydro[1,3,5]triazino[1,2-a]benzimidazol-2-amine (IC50 = 10.9 microM). 2007 Journal Article http://hdl.handle.net/20.500.11937/16544 10.1007/s11094-007-0103-5 Springer restricted |
| spellingShingle | Dolzhenko, Anton Chui, W. Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines. |
| title | Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines. |
| title_full | Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines. |
| title_fullStr | Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines. |
| title_full_unstemmed | Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines. |
| title_short | Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines. |
| title_sort | synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines. |
| url | http://hdl.handle.net/20.500.11937/16544 |