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dc.contributor.authorWilkinson, Brendan L
dc.contributor.authorBornaghi, Laurent F
dc.contributor.authorPoulsen, Sally-Ann
dc.contributor.authorHouston, Todd A
dc.date.accessioned2017-05-03T11:45:26Z
dc.date.available2017-05-03T11:45:26Z
dc.date.issued2006
dc.date.modified2007-12-24T03:55:26Z
dc.identifier.issn0065-7727
dc.identifier.urihttp://hdl.handle.net/10072/16282
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.
dc.description.publicationstatusYes
dc.languageEnglish
dc.language.isoeng
dc.publisherAmerican Chemical Society
dc.publisher.placeWashington, D. C.
dc.publisher.urihttp://acswebcontent.acs.org/nationalmeeting/atlanta2006/home.html
dc.relation.ispartofstudentpublicationN
dc.relation.ispartofconferencename231st National Meeting of the American-Chemical-Society
dc.relation.ispartofconferencetitleABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY
dc.relation.ispartofdatefrom2006-03-26
dc.relation.ispartofdateto2006-03-30
dc.relation.ispartoflocationAtlanta, GA
dc.relation.ispartofpagefrom1 pages
dc.relation.ispartofpageto1 pages
dc.relation.ispartofvolume231
dc.rights.retentionN
dc.subject.fieldofresearchcode250302
dc.titleIn situ click synthesis of glycosyltriazole arylsulfonamides: Hydrophilic carbonic anhydrase II inhibitors.
dc.typeConference output
dc.type.descriptionE3 - Conferences (Extract Paper)
dc.type.codeE - Conference Publications
gro.facultyGriffith Sciences, School of Natural Sciences
gro.date.issued2006
gro.hasfulltextNo Full Text
gro.griffith.authorPoulsen, Sally-Ann
gro.griffith.authorHouston, Todd A.


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

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