Purine analogues as amplifiers of phleomycin. III. Some 2-alkylthio derivatives of imidazole, benzimidazole, benzoxazole and benzothiazole

Abstract

Some 2-methylthio and 2-carbamoylalkylthio derivatives of 1-methylimidazole, benzimidazole, benzoxazole, benzothiazole and 6-dimethylaminobenzothiazole have been synthesized by alkylation of the corresponding thiones. Their in vitro activities, as amplifiers of phleomycin against Escherichia coli, varied from slight to high but none was outstanding. 2-(Benzothiazol-2'-ylthio)acetamide (2j)showed maximal activity at c. 0.04 mM with progressive decreases at both higher and lower concentrations.