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Elsevier, Bioorganic and Medicinal Chemistry Letters, 21(19), p. 6014-6017, 2009

DOI: 10.1016/j.bmcl.2009.09.047

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Carbonic anhydrase II-induced selection of inhibitors from a dynamic combinatorial library of Schiff's bases

Journal article published in 2009 by Gihane Nasr, Eddy Petit, Ct-T. Supuran, Jean-Yves Winum ORCID, Mihai Barboiu ORCID
This paper is available in a repository.
This paper is available in a repository.

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Abstract

, DOI = 10.1016/j.bmcl.2009.09.047 ; International audience ; A dynamic combinatorial library (DCL) has been generated under thermodynamic control by using the aminocarbonyl/imine interconversion as reversible chemistry, combined with non-covalent binding within the active site of the metalloenzyme human carbonic anhydrase II (hCA II, EC 4.2.1.1). The high affinity of hCA II isozyme towards some sulfonamide inhibitors obtained here was used to select from the dynamic library specific inhibitors of this isoform. These results point out to the possibility of identifying sulfonamide amplified compounds presenting potent inhibition and high yield of formation in the presence of the isoform(s) towards which the inhibitors were designed.