Abstract

In search for new antibiotics we replaced the amide moiety of lincomycin 1 by a 1,2,3-triazole ring. The 1,2,3-triazoles 10a – 10k were obtained as single regioisomers by 9click reaction: of azide 5 with the alkyne 9k, derived from propyl hygric acid, and the alkyl, aryl, or cycloalkyl alkynes ribosomes 9a – 9j. The new analogues proved inactive towards wild-type and A2058G mutant.