81187-93-1Relevant articles and documents
Dihydropyrrolones as bacterial quorum sensing inhibitors
Almohaywi, Basmah,Yu, Tsz Tin,Iskander, George,Chan, Daniel S.H.,Ho, Kitty K.K.,Rice, Scott,Black, David StC.,Griffith, Renate,Kumar, Naresh
supporting information, p. 1054 - 1059 (2019/03/13)
Bacteria regulate their pathogenicity and biofilm formation through quorum sensing (QS), which is an intercellular communication system mediated by the binding of signaling molecules to QS receptors such as LasR. In this study, a range of dihydropyrrolone (DHP) analogues were synthesized via the lactone-lactam conversion of lactone intermediates. The synthesized compounds were tested for their ability to inhibit QS, biofilm formation and bacterial growth of Pseudomonas aeruginosa. The compounds were also docked into a LasR crystal structure to rationalize the observed structure-activity relationships. The most active compound identified in this study was compound 9i, which showed 63.1% QS inhibition of at 31.25 μM and 60% biofilm reduction at 250 μM with only moderate toxicity towards bacterial cell growth.
Synthesis and Structure-Activity Relationships of Tambjamines and B-Ring Functionalized Prodiginines as Potent Antimalarials
Kancharla, Papireddy,Kelly, Jane Xu,Reynolds, Kevin A.
, p. 7286 - 7309 (2015/10/05)
Synthesis and antimalarial activity of 94 novel bipyrrole tambjamines (TAs) and a library of B-ring functionalized tripyrrole prodiginines (PGs) against a panel of Plasmodium falciparum strains are described. The activity and structure-activity relationsh
Synthesis of analogues of GABA. VIII. (Z)- and (E)-4-amino-3-(4-chlorophenyl)but-2-enoic acids as unsaturated baclofen derivatives
Allan,Tran
, p. 2641 - 2645 (2007/10/02)
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