Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:2.3.1.184 (
LasR
)
897
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Emergence of multi-drug resistant bacterial pathogens is escalating and it is essential to develop novel strategies to combat these super bugs.
LasR
is a regulator switch that plays a vital role in quorum sensing (QS) and pathogenesis of Pseudomonas aeruginosa. The present study reports two novel Mannich base (1-(phenyl (o-tolylamino) methyl) urea and 3-((
1H-Imidazole
-1-yl) methylnaphthalene-2-ol with enhanced anti-QS and antibiofilm activities. Synthetic compound revealed prolific interaction patterns with
LasR
quorum sensing receptor and showed to exhibit
LasR
antagonistic activities in P. aeruginosa. In-vitro
LasR
-inhibitory activities were further confirmed by biofilm and pyocyanin inhibition assays which showed a dose-dependent activity. The Mannich base also repressed the mRNA transcripts levels of lasA and lasB genes, confirming its active role in
LasR
inhibitory activity. Importantly, C1 and C2 played a crucial role in antagonizing
LasR
receptor by forming H-bonds with Tyr
47
in the
LasR
active site and the presence of urea moiety on one of the Mannich base was a discrete advantage. Taken together, the insilico and invitro assays revealed similar evidences, thus confirming the mode of action of the Mannich bases. Overall the findings will assist in drug designing and for developing newer drugs with Mannich bases and its derivatives for treatment of P. aeruginosa.
...
PMID:Molecular docking and biological evaluation of novel urea-tailed mannich base against Pseudomonas aeruginosa. 3084 91
