In situ click synthesis of glycosyltriazole arylsulfonamides: Hydrophilic carbonic anhydrase II inhibitors.

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Title In situ click synthesis of glycosyltriazole arylsulfonamides: Hydrophilic carbonic anhydrase II inhibitors.
Author Wilkinson, Brendan Luke; Bornaghi, Laurent; Poulsen, Sally-Ann; Houston, Todd Ashley
Publication Title Abstracts of Papers, 231st ACS National Meeting, Atlanta, GA, United States, March 26-30, 2006.
Year Published 2006
Place of publication Washington, D. C.
Publisher American Chemical Society
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 ß-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.
Peer Reviewed No
Published Yes
Publisher URI http://acswebcontent.acs.org/nationalmeeting/atlanta2006/home.html
Conference name 231st ACS National Meeting
Location Atlanta, GA, United States
Date From 2006-03-26
Date To 2006-03-30
URI http://hdl.handle.net/10072/16282
Date Accessioned 2007-03-14
Date Available 2007-12-24T03:55:26Z
Language en_AU
Research Centre Eskitis Institute for Drug Discovery; Institute for Glycomics
Faculty Faculty of Science, Environment, Engineering and Technology
Subject Biological and Medical Chemistry
Publication Type Conference Publications (Extract Paper)
Publication Type Code e3

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