Anti-Candida activity of four antifungal benzothiazoles

Abstract

Anti-Candida activity of 6-amino-2-n-pentylthiobenzothiazole (I), benzylester of (6-amino-2-benzothiazolylthio)acetic acid (II) and of 3-butylthio-(1,2,4-triazolo)-2,3-benzothiazole (III) was followed and compared to that of 2-mercaptobenzothiazole (IV). I and II exhibited good activity against the C. albicans yeast form, similar to IV. They were inhibitorily active against other Candida strains, IC50 values being of the order of 10(-5) M, which means better activity than IV. Compound I also exhibited inhibitory activity on germ-tube formation and mycelial growth in the C. albicans strains, while II, III and IV were not active in these tests. III was the least active form of the compounds tested, IC50 values being of the order of 10(-4) M. All the compounds tested were highly active on a nystatin-resistant C. albicans mutant, with IC50s of the order of 10(-6) M-10(-5) M.