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dc.contributor.authorWilkinson, Brendanen_US
dc.contributor.authorBornaghi, Laurenten_US
dc.contributor.authorPoulsen, Sally-Annen_US
dc.contributor.authorHouston, Todden_US
dc.description.abstractThe Carbonic anhydrase (CA) family of hydrolytic Zn(II) metalloenzymes are ubiquitous to all eukaryotic and prokaryotic cells.[1] For decades, aryl sulfonamides have been a mainstay of clinical intervention as antibacterial agents, but only more recently have sulfonamide CA inhibitors been investigated for their anti-cancer and anti-glaucoma activities.[1,2] Recently, Supuran and coworkers have synthesized and evaluated the activity of a series of ߭glycosyl sulfonamides as topical anti-glaucoma agents in rabbit models with high intra ocular pressures (IOP).[2] Within this study, we have developed a new class of hydrophilic aryl sulfonamides with potential anti-glaucoma activity using the in situ click chemistry approach.[3] Screening of the library was achieved using a flouresent DNSA assay, as well as in situ in the presence of the enzyme using a bioaffinity characterization mass spectrometry (BACMS) methodology.[4] Inhibition constants (Ki's) were found to be in the mid to low nM range for bCAII, comparable to the in vitro activity of current treatments of glaucoma.en_US
dc.publisherAmerican Chemical Societyen_US
dc.publisher.placeWashington, D. C.en_US
dc.relation.ispartofconferencename231st ACS National Meetingen_US
dc.relation.ispartofconferencetitleAbstracts of Papers, 231st ACS National Meeting, Atlanta, GA, United States, March 26-30, 2006.en_US
dc.relation.ispartoflocationAtlanta, GA, United Statesen_US
dc.titleIn situ click synthesis of glycosyltriazole arylsulfonamides: Hydrophilic carbonic anhydrase II inhibitors.en_US
dc.typeConference outputen_US
dc.type.descriptionE3 - Conference Publications (Extract Paper)en_US
dc.type.codeE - Conference Publicationsen_US
gro.facultyGriffith Sciences, School of Natural Sciencesen_US
gro.hasfulltextNo Full Text

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    Contains papers delivered by Griffith authors at national and international conferences.

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