Oligoamides of 2-amino-5-alkylthiazole 4-carboxylic acids : anti-trypanosomal compounds

Lang, Stuart and Khalaf, Abedawn I and Breen, David and Huggan, Judith and Clements, Carol and MacKay, Simon and Suckling, Colin (2014) Oligoamides of 2-amino-5-alkylthiazole 4-carboxylic acids : anti-trypanosomal compounds. Medicinal Chemistry Research, 23 (3). pp. 1170-1179.

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Abstract

A range of minor groove binders (MGBs) and the intermediates formed in their synthesis was screened against infectious agents including bacteria and parasites. Activity was found against Trypanosoma brucei. Of particular interest is a molecule which does not contain a typical basic flexible tail group found in MGBs, but instead has an unprotected carboxylic acid group at that position (compound 4), which has activity of 63 nM against T. brucei.