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Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2009

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

Gihane Nasr
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Eddy Petit
Ct. Supuran
  • Fonction : Auteur
Jy. Winum
  • Fonction : Auteur
Mihai Barboiu

Résumé

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

Dates et versions

hal-00426709 , version 1 (27-10-2009)

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Gihane Nasr, Eddy Petit, Ct. Supuran, Jy. Winum, Mihai Barboiu. Carbonic anhydrase II-induced selection of inhibitors from a dynamic combinatorial library of Schiff's bases. Bioorganic and Medicinal Chemistry Letters, 2009, 19 (21), pp.6014 - 6017. ⟨10.1016/j.bmcl.2009.09.047⟩. ⟨hal-00426709⟩
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