In vitro studies of antimicrobial activity of Gly-His-Lys conjugates as potential and promising candidates for therapeutics in skin and tissue infections.
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| Abstract |
In this Letter, we presented in vitro studies of antimicrobial activity of Gly-His-Lys conjugates that are important point in preliminary biological evaluation of their potential application in skin and tissue therapies. The novel compounds include the conjugation of fatty acids with a modification of the amino acid sequence in the primary structure of Gly-His-Lys (6i). All the compounds exhibited strong to moderate activity. Compound 1d had the most potent antimicrobial activity at MIC ranges 31.3-125.0μg/mL (against Escherichia coli spp. and Staphylococcus aureus spp.), 375.0-500.0μg/mL (against Pseudomonas aeruginosa spp.). Conjugate 5b expressed activity against Staphylococcus aureus spp. and Escherichia coli spp. at MIC ranges 250.0-500.0μg/mL and 62.5-125.0μg/mL, respectively. Both conjugates 1d and 5b possessed rapid bactericidal activity against Gram-positive bacteria at 2MIC or 4MIC. Conjugates 1b-c, 1e, 2a-b and 4b showed noticeable effect against both Gram-positive and Gram-negative bacteria. Compounds 1d, 1e and 2e were the most active against fungus.
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| Authors | Monika Kukowska, Magdalena Kukowska-Kaszuba, Krystyna Dzierzbicka |
| Journal | Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 25 Issue 3 Pg. 542-6 (Feb 01 2015) ISSN: 1464-3405 [Electronic] England |
| PMID | 25556094 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't) |
| Copyright | Copyright © 2014 Elsevier Ltd. All rights reserved. |
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