Anti-bacterial glycosyl triazoles - Identification of an N-acetylglucosamine derivative with bacteriostatic activity against Bacillus.

摘要: N-Acetylglucosaminidases (GlcNAcases) play an important role in the remodeling and recycling of bacterial peptidoglycan. Inhibitors GlcNAcases can serve as antibacterial agents provide opportunity for development new antibiotics. We report synthesis triazole derivatives N-acetylglucosamine using a copper promoted azide–alkyne coupling reaction between 1-azido-N-acetylglucosamine small library terminal alkynes prepared via Ugi reaction. These compounds were evaluated their ability to inhibit growth bacteria. Two that show bacteriostatic activity against Bacillus identified, with MIC values approximately 60 μM both cases. subtilis cultured presence sub-MIC amounts glycosyl inhibitors exhibit elongated phenotype characteristic impaired cell division. This represents first wall demonstrate inhibition whole assays.