Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides.

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Holmes JM, Lee GC, Wijono M, Weinkam R, Wheeler LA, Garst ME

Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides.

J Med Chem. 1994 May 27;37(11):1646-51.

PubMed ID

8201598 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Acetazolamide	Carbonic anhydrase 2	IC 50 (nM)	6	N/A	N/A	Details