Novel synthetic analogs of the Pseudomonas autoinducer

T Kline, J Bowman, BH Iglewski, T De Kievit… - Bioorganic & medicinal …, 1999 - Elsevier
T Kline, J Bowman, BH Iglewski, T De Kievit, Y Kakai, L Passador
Bioorganic & medicinal chemistry letters, 1999Elsevier
Release of virulence factors in Pseudomonas aeruginosa is regulated by two N-
acylhomoserine lactones, PAI-1 and PAI-2, that activate the respective transcription factors
LasR and RhlR. With the goal of developing novel therapeutic agents, we synthesized
constrained analogs of PAI-1 and evaluated them in P. aeruginosa. Two of the novel
analogs bound to LasR and showed agonist activity in LasR stimulation of a lasI-lacZ
reporter construct.
Release of virulence factors in Pseudomonas aeruginosa is regulated by two N-acylhomoserine lactones, PAI-1 and PAI-2, that activate the respective transcription factors LasR and RhlR. With the goal of developing novel therapeutic agents, we synthesized constrained analogs of PAI-1 and evaluated them in P. aeruginosa. Two of the novel analogs bound to LasR and showed agonist activity in LasR stimulation of a lasI-lacZ reporter construct.
Elsevier