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Antibacterial and Antibiofilm Activity of Cationic Small Molecules with Spatial Positioning of Hydrophobicity: An in Vitro and in Vivo Evaluation

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dc.contributor.author Hoque, Jiaul
dc.contributor.author Konai, Mohini M.
dc.contributor.author Sequeira, Shanola S.
dc.contributor.author Samaddar, Sandip
dc.contributor.author Haldar, Jayanta
dc.date.accessioned 2017-01-24T09:11:14Z
dc.date.available 2017-01-24T09:11:14Z
dc.date.issued 2016
dc.identifier.citation Hoque, J.; Konai, M. M.; Sequeira, S. S.; Samaddar, S.; Haldar, J., Antibacterial and Antibiofilm Activity of Cationic Small Molecules with Spatial Positioning of Hydrophobicity: An in Vitro and in Vivo Evaluation. Journal of Medicinal Chemistry 2016, 59 (23), 10750-10762 http://dx.doi.org/10.1021/acs.jmedchem.6b01435 en_US
dc.identifier.citation Journal of Medicinal Chemistry en_US
dc.identifier.citation 59 en_US
dc.identifier.citation 23 en_US
dc.identifier.issn 0022-2623
dc.identifier.uri https://libjncir.jncasr.ac.in/xmlui/10572/2305
dc.description Restricted Access en_US
dc.description.abstract More than 80% of the bacterial infections are associated with biofilm formation. To combat infections, amphiphilic small molecules have been developed as promising antibiofilm agents. However, cytotoxicity of such molecules still remains a major problem. Herein we demonstrate a concept in which antibacterial versus cytotoxic activities of cationic small molecules are tuned by spatial positioning of hydrophobic moieties while keeping positive charges constant. Compared to the molecules with more pendent hydrophobicity from positive centers (MIC = 1-4 mu g/mL and HC50 = 60-65 mu g/mL), molecules with more confined hydrophobicity between two centers show similar antibacterial activity but significantly less toxicity toward human erythrocytes (MIC = 1-4 mu g/mL and HC50 = 805-1242 mu g/mL). Notably, the optimized molecule is shown to be nontoxic toward human cells (HEK 293) at a concentration at which it eradicates established bacterial biofilms. The molecule is also shown to eradicate preformed bacterial biofilm in vivo in a murine model of superficial skin infection. en_US
dc.description.uri 1520-4804 en_US
dc.description.uri http://dx.doi.org/10.1021/acs.jmedchem.6b01435 en_US
dc.language.iso English en_US
dc.publisher American Chemical Society en_US
dc.rights @American Chemical Society, 2016 en_US
dc.subject Pharmacology & Pharmacy en_US
dc.subject Biofilm Formation en_US
dc.subject Pseudomonas-Aeruginosa en_US
dc.subject Antimicrobial Peptides en_US
dc.subject Bacterial Biofilms en_US
dc.subject Amphiphilic Polymers en_US
dc.subject Eradicate Biofilms en_US
dc.subject Swarming Motility en_US
dc.subject Side-Chain en_US
dc.subject Inhibition en_US
dc.subject Resistance en_US
dc.title Antibacterial and Antibiofilm Activity of Cationic Small Molecules with Spatial Positioning of Hydrophobicity: An in Vitro and in Vivo Evaluation en_US
dc.type Article en_US


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