公开(公告)号：US11247976B2

公开(公告)日：2022-02-15

申请号：US16097541

申请日：2017-04-30

Applicant: Wisconsin Alumni Research Foundation

Inventor： Helen Blackwell ,  Michelle E. Boursier ,  Joseph D. Moore

IPC: C07D307/33 ,  C07D333/36 ,  C07D207/09 ,  C07D207/273 ,  C07D307/14 ,  C07C233/06 ,  C07C233/61 ,  C07C235/22 ,  C07C201/00 ,  C07D307/22 ,  C07C233/58 ,  C07C233/60 ,  C07C233/32

Abstract: RhlR modulators including agonist and antagonists which are useful for modulating QS phenotypes in Gram-negative bacteria. Certain compounds of general formula A-W-HG having various carbocyclic ad heterocyclic head groups (HG) and various tail groups (A), where —W— is —CO—NH—, —SO2—NH—, —CO—NH—CH2—, or —SO2—NH—CH2— are RhlR agonists or antagonists. The compounds are useful in methods of modulating quorum sensing in Gram-negative bacteria, particularly in Pseudomonas. Compositions including certain RhlR modulators are useful for decreasing the virulence of Gram-negative bacteria. Pharmaceutical compositions comprising certain RhlR modulators are useful for treatment of infections of Gram-negative bacteria.