Cationic chalcone antibiotics. Design, synthesis, and mechanism of action

…, T Boesen, K Schønning, H Kromann

Index: Nielsen, Simon F.; Larsen, Mogens; Boesen, Thomas; Schonning, Kristian; Kromann, Hasse Journal of Medicinal Chemistry, 2005 , vol. 48, # 7 p. 2667 - 2677

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Citation Number: 116

Abstract

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 ...