Cationic chalcone antibiotics. Design, synthesis, and mechanism of action
This paper describes how the introduction of "cationic" aliphatic amino groups in the chalcone scaffold results in potent antibacterial compounds. It is shown that the most favorable position for the aliphatic amino group is the 2-position of the B-ring, in particular in combination with a lipophilic substituent in the 5-position of the B-ring. We demonstrate that the compounds act by unselective disruption of cell membranes. Introduction of an additional aliphatic amino group in the á-ring results in compounds that are selective for bacterial membranes combined with a high antibacterial activity against both Gram-positive and -negative pathogens. The most potent compound in this study (78) has an MIC value of 2 μM against methicillin resistant Staphylococus aureus.
Nielsen, Simon F.,Larsen, Mogens,Boesen, Thomas,Sch?nning, Kristian,Kromann, Hasse
p. 2667 - 2677
(2007/10/03)
A NEW REGIOSPECIFIC SYNTHESIS OF ARYL KETONES FROM PALLADOCYCLES
Aromatic palladocycles undergo facile reaction with acid halides to regiospecifically provide aryl ketones in high yield.
Holton, R. A.,Natalie, K. J.
p. 267 - 270
(2007/10/02)
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