Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines.

Dolzhenko, Anton; Chui, W.

doi:10.1007/s11094-007-0103-5

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Authors

Dolzhenko, Anton

Chui, W.

Date

2007

Type

Journal Article

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Citation

Dolzhenko, Anton and Chui, Wai. 2007. Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2-amines. Pharmaceutical Chemistry Journal. 41 (9): pp. 470-473.

Source Title

Pharmaceutical Chemistry Journal

DOI

10.1007/s11094-007-0103-5

ISSN

0091-150X

School

School of Pharmacy

URI

http://hdl.handle.net/20.500.11937/16544

Collection

Curtin Research Publications

Abstract

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).