N-cholesteryl amino acid conjugates and their antimicrobial activities

A series of N-cholesteryl amino acid conjugates have been synthesized using a reductive amination protocol in good yield and purity. All the synthesized conjugates were evaluated for their in vitro antimicrobial activities against Gram positive and Gram negative bacteria. Among the conjugates tested, N-cholesteryl GABA 12 showed the highest potency toward the methicillin-resistant Staphylococcus aureus with the lowest MIC value of 2 μg/mL. Hemolytic activities of the compounds 3, 4, 11, and 12 were determined. All compounds tested had no significant hemolytic activity up to >50 μg/mL.

Graphical abstractA series of N-cholesteryl amino acid conjugates have been synthesized using a reductive amination protocol in good yield and purity. N-Cholesteryl GABA conjugate 12 showed the highest potency toward the Gram positive strain S. aureus with the lowest MIC value of 2 μg/mL.Download high-res image (106KB)Download full-size image