Dérivés de l'imidazo[2,1- b]thiazole X. Propriétés fongistatiques de 2-aminothiazoles et de 6-aryl imidazo[2,1- b]thiazoles substitués respectivement en 4 et en 3 par un reste aryléthyle, aroylméthyle, [formula omitted] et éthoxycarbonylméthyle

Abstract

Several 2-aminothiazoles, substituted in 4 with an ethylacetate, aroylmethyl, β-hydroxy β-arylethyl or arylethyl chain, were combined with ω-bromoacetophenones in order to obtain the corresponding 3-substituted 6-arylimidazo[2,1- b]thiazoles to perform fungi-static tests. The ethyl (2-aminothiazole-4-yl) acetates led to the expected imidazothiazoles. This was not noted in the other cases. Thus, the presence of an aroylmethyl residue considerably decrease the reactivity of the aminothiazole. The transformation of the ketonic carbonyl to alcohol II, or even better, to methylene is necessary for the condensation to be effected with ω-bromoacetophenones. The yield of this reaction is low. The results of fungistatic tests show the interest of the aminothiazole derivatives with an aroylmethyl on Candida albicans, Aspergillus fumigatus, Epidermophyton floccosum. The best activity is observed when the phenyl has one or several methyl or methoxy groups. The imidazothiazole compounds, although there is a substitution in 6, show lower efficiency.