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Eur J Pharm Sci. 2013 Oct 9;50(2):208-14. doi: 10.1016/j.ejps.2013.07.005. Epub 2013 Jul 18.

N-cholesteryl amino acid conjugates and their antimicrobial activities.

Author information

  • 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.

Copyright © 2013 Elsevier B.V. All rights reserved.

KEYWORDS:

Antimicrobial agents; Methicillin-resistant Staphylococcus aureus; N-Cholesteryl amino acid conjugates; SAR study

PMID:
23872625
[PubMed - indexed for MEDLINE]
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