dc.contributor.author | Wilkinson, Brendan L | |
dc.contributor.author | Bornaghi, Laurent F | |
dc.contributor.author | Poulsen, Sally-Ann | |
dc.contributor.author | Houston, Todd A | |
dc.date.accessioned | 2017-05-03T11:45:26Z | |
dc.date.available | 2017-05-03T11:45:26Z | |
dc.date.issued | 2006 | |
dc.date.modified | 2007-12-24T03:55:26Z | |
dc.identifier.issn | 0065-7727 | |
dc.identifier.uri | http://hdl.handle.net/10072/16282 | |
dc.description.abstract | The 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.publicationstatus | Yes | |
dc.language | English | |
dc.language.iso | eng | |
dc.publisher | American Chemical Society | |
dc.publisher.place | Washington, D. C. | |
dc.publisher.uri | http://acswebcontent.acs.org/nationalmeeting/atlanta2006/home.html | |
dc.relation.ispartofstudentpublication | N | |
dc.relation.ispartofconferencename | 231st National Meeting of the American-Chemical-Society | |
dc.relation.ispartofconferencetitle | ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY | |
dc.relation.ispartofdatefrom | 2006-03-26 | |
dc.relation.ispartofdateto | 2006-03-30 | |
dc.relation.ispartoflocation | Atlanta, GA | |
dc.relation.ispartofpagefrom | 1 pages | |
dc.relation.ispartofpageto | 1 pages | |
dc.relation.ispartofvolume | 231 | |
dc.rights.retention | N | |
dc.subject.fieldofresearchcode | 250302 | |
dc.title | In situ click synthesis of glycosyltriazole arylsulfonamides: Hydrophilic carbonic anhydrase II inhibitors. | |
dc.type | Conference output | |
dc.type.description | E3 - Conferences (Extract Paper) | |
dc.type.code | E - Conference Publications | |
gro.faculty | Griffith Sciences, School of Natural Sciences | |
gro.date.issued | 2006 | |
gro.hasfulltext | No Full Text | |
gro.griffith.author | Poulsen, Sally-Ann | |
gro.griffith.author | Houston, Todd A. | |