Design and Synthesis of Imidazo[1,2‐a]pyridines with Carboxamide Group Substitution and In silico Evaluation of their Interaction with a LuxR‐type Quorum Sensing Receptor

Quorum sensing, an important process of bacterial communication, is involved in the development of complex behavior and expression of virulence factors that become important due to its key role in infection process. In this manuscript, docking studies were used as a preliminary screening to identify...

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Bibliographic Details
Published in:Journal of heterocyclic chemistry 2018-05, Vol.55 (5), p.1101-1111
Main Authors: Reynoso Lara, Juan Emmanuel, Salgado‐Zamora, Héctor, Bazin, Marc‐Antoine, Campos‐Aldrete, María Elena, Marchand, Pascal
Format: Article
Language:English
Subjects:
Biological activity
Detection
Docking
Lactones
Molecular chains
Pyridines
Urea
Virulence
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Summary:Quorum sensing, an important process of bacterial communication, is involved in the development of complex behavior and expression of virulence factors that become important due to its key role in infection process. In this manuscript, docking studies were used as a preliminary screening to identify main interactions between LuxR receptor (CviR) of Chromobacterium violaceum as model and N‐acyl L‐homoserine lactones. Thus, following this approach, a library of imidazo[1,2‐a]pyridines bearing carboxamide and urea moieties was designed, evaluated on this in silico model previously validated, and synthesized to generate new potential quorum sensing inhibitors. The present article summarizes survey to develop these new molecules with potential biological activity, based on interaction analysis ligand‐receptor.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.3140