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Effect of replacing main-chain ureas with thiourea and guanidinium surrogates on the bactericidal activity of membrane active oligourea foldamers

hal.structure.identifierChimie et Biologie des Membranes et des Nanoobjets [CBMN]
dc.contributor.authorANTUNES, Stephanie
dc.contributor.authorCORRE, Jean-Philippe
dc.contributor.authorMIKATY, Guillain
hal.structure.identifierChimie et Biologie des Membranes et des Nanoobjets [CBMN]
dc.contributor.authorDOUAT, Celine
dc.contributor.authorGOOSSENS, Pierre L.
hal.structure.identifierChimie et Biologie des Membranes et des Nanoobjets [CBMN]
dc.contributor.authorGUICHARD, Gilles
IDREF: 084339268
dc.date.accessioned2020-07-09T14:17:17Z
dc.date.available2020-07-09T14:17:17Z
dc.date.issued2017-08-15
dc.identifier.issn0968-0896
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/10366
dc.description.abstractEnMembrane-active foldamers have recently emerged as potential mimics of antimicrobial peptides (AMPs). Amphiphilic cationic helical N,N'-linked oligoureas are one such class of AMP mimics with activities in vitro against a broad range of bacteria including Bacillus anthracis, a Gram-positive sporulating bacillus and causing agent of anthrax. Here we have used site-selective chemical modifications of the oligourea backbone to gain additional insight into the relationship between structure and function and modulate anthracidal activity. A series of analogues in which urea linkages at selected positions are replaced by thiourea and guanidium surrogates have been prepared on solid support and tested against different bacterial forms of B. anthracis (germinated spores and encapsulated bacilli). Urea ? thiourea and urea? guanidinium replacements close to the negative end of the helix dipole led to analogues with increased potency and selectivity for B. anthracis versus mammalian cells. (C) 2017 Elsevier Ltd. All rights reserved.
dc.title.enEffect of replacing main-chain ureas with thiourea and guanidinium surrogates on the bactericidal activity of membrane active oligourea foldamers
dc.typeArticle de revue
dc.identifier.doi10.1016/j.bmc.2017.04.040
dc.subject.halChimie/Matériaux
bordeaux.journalBioorganic & Medicinal Chemistry
bordeaux.page4245-4252
bordeaux.volume25
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN) - UMR 5248*
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN, UMR 5248)
bordeaux.issue16
bordeaux.institutionUniversité de Bordeaux
bordeaux.institutionBordeaux INP
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Bioorganic%20&%20Medicinal%20Chemistry&rft.date=2017-08-15&rft.volume=25&rft.issue=16&rft.spage=4245-4252&rft.epage=4245-4252&rft.eissn=0968-0896&rft.issn=0968-0896&rft.au=ANTUNES,%20Stephanie&CORRE,%20Jean-Philippe&MIKATY,%20Guillain&DOUAT,%20Celine&GOOSSENS,%20Pierre%20L.&rft.genre=article


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