Bioorganic and Medicinal Chemistry Letters p. 3447 - 3452 (1999)
Update date:2022-08-04
Topics:
Kline
Bowman
Iglewski
De Kievit
Kakai
Passador
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 Rh1R. 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.
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