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N-cholesteryl amino acid conjugates and their antimicrobial activities
Jyoti R Jadhav1, Hong-Seok Kim, Jin-Hwan Kwak
1Department of Applied Chemistry, Kyungpook National University, Daegu 702-701, Republic of Korea.
Abstract:
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.
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