Background: Antibiotic resistance is a growing threat in the treatment of
bacterial diseases. Bacterial invasion and its virulence can cause damage to the host
cells via quorum sensing mechanism which is responsible for the intercellular communication
among bacteria that regulates expression of many genes. Quorum sensing
(QS) differentially expresses specific sets of genes which may produce resistance.
Researchers have been devoted to develop more potent compounds against
bacterial resistant quorum sensing inhibitors.
Methods: A number of anti-quorum sensing approaches have been documented to
screen potent inhibitors against quorum sensing induced bacterial virulence. Experimental
screening of a large chemical compound library against a quorum sensing biological target is an
established technology for lead identification but it is expensive, laborious and time consuming. Therefore,
computer-aided high throughput ligand and structure based virtual screening are most effective
pharmacoinformatic tools prior to experiment in this context.
Results: Ligand based screening includes quantitative structure-activity relationship (QSAR) and pharmacophore
generation whereas techniques of structure based virtual screening include molecular docking.
The study in this direction can increase the findings of hit rates and decrease cost of drug design
and development by producing potent natural as well as synthetic anti-quorum sensing compounds.
Conclusion: Most recent patent coverage on ligand and structure based design of novel bioactive quorum
sensing inhibitors has been presented here. The paper has also critically reviewed the screening and
design of potent quorum sensing inhibitor leads that would help in patenting novel leads active against
bacterial virulence and minimizing antibiotic resistance among bacterial pathogens.