O'Brien Kevin T, Noto Joseph G, Nichols-O'Neill Luke, Perez Lark J
Department of Chemistry and Biochemistry, Rowan University , 201 Mullica Hill Road, Glassboro, New Jersey 08028, United States.
ACS Med Chem Lett. 2014 Dec 27;6(2):162-7. doi: 10.1021/ml500459f. eCollection 2015 Feb 12.
Antagonism of quorum sensing represents a promising new antivirulence approach for the treatment of bacterial infection. The development of a novel series of non-natural irreversible antagonists of P. aeruginosa LasR is described. The lead compounds identified (25 and 28) display potent LasR antagonist activity and inhibit expression of the P. aeruginosa virulence factors pyocyanin and biofilm formation in PAO1 and PA14.
群体感应拮抗作用是一种用于治疗细菌感染的有前景的新型抗毒力方法。本文描述了一系列新型铜绿假单胞菌LasR非天然不可逆拮抗剂的研发情况。所鉴定出的先导化合物（25和28）表现出强大的LasR拮抗活性，并抑制铜绿假单胞菌毒力因子绿脓菌素的表达以及PAO1和PA14中生物膜的形成。
