Synthesis and antimicrobial activity of some netropsin analogues |
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Authors: | Khalaf Abedawn I Ebrahimabadi Abdolrasoul H Drummond Allan J Anthony Nahoum G Mackay Simon P Suckling Colin J Waigh Roger D |
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Affiliation: | Department of Pure and Applied Chemistry, University of Strathclyde, Glasgow, Scotland, UKG1 1XL. abedawn.khalaf@strath.ac.uk |
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Abstract: | Nine novel lexitropsins were synthesized by linking two netropsin-like moieties through three different dicarboxylic acids; 9,10-dihydro-2,7-phenanthrenedicarboxylic acid; [(3-[[(carboxymethyl)amino]carbonyl]benzoyl)amino]acetic acid and indole-2,5-dicarboxylic acid. The netropsin residues were modified by the use of N-isopentylpyrrole, 5-methylthiophene or 5-isopropylthiazole heterocyclic building blocks in place of the usual N-methylpyrrole. The compounds were tested against five gram-positive bacteria: Staphylococcus aureus, Streptomyces faecalis, methicillin resistant Staphylococcus aureus, Enterobacter cloacae, Mycobacterium fortuitum, three gram-negative bacteria: Klebsiella aerogenes, Proteus vulgaris, Escherichia coli and three fungi: Aspergillus niger, Candida albicans and Aspergillus nidulans. Some of the compounds showed significant inhibitory effects on the growth of the microorganisms. |
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