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Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides
J M Holmes1, G C Lee, M Wijono
1Department of Chemical Sciences, Allergan Inc., Irvine, California 92715.
Journal of Medicinal Chemistry
|May 27, 1994
Abstract:
A series of 4-substituted 2-thiophenesulfonamides was prepared from 3-thiophenecarboxaldehyde using metalation chemistry developed for 3-furaldehyde. Several of these compounds inhibit carbonic anhydrase II in vitro at concentrations of less than 10 nM. In addition, none of these compounds exhibit sensitization potential as determined from in vitro measurement of cysteine reactivity.