期刊
CHEMBIOCHEM
卷 9, 期 8, 页码 1267-1279出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.200700774
关键词
biological activity; drug design; medicinal chemistry; natural products; structure-activity relationships
A 50-compound library based on the marine natural product oroidin was synthesized and assayed for anti-biofilm activity against PAO1 and PA14, two strains of the medically relevant gamma-proteobacterium Pseudomonas aeruginosa. Through structure-activity relationship (SAR) analysis of analogues based on the oroidin template, several conclusions can be drawn as to what structural properties of the synthetic derivatives are necessary to elicit a biological response. Notably, the most active analogues identified were those that contained a 2-aminoimidazole (2-Al) motif and a dibrominoted pyrrolecarboxamide subunit. Here we disclose the synthesis and subsequently determined biological activity of this unique class of compounds as inhibitors of biofilm formation that have no direct antibiotic effect.
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