4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII.

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Sudzius J, Baranauskiene L, Golovenko D, Matuliene J, Michailoviene V, Torresan J, Jachno J, Sukackaite R, Manakova E, Grazulis S, Tumkevicius S, Matulis D

4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII.

Bioorg Med Chem. 2010 Nov 1;18(21):7413-21. doi: 10.1016/j.bmc.2010.09.011. Epub 2010 Sep 8.

PubMed ID

20889345 [ View in PubMed

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Abstract

A series of 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides were designed and synthesised. Their binding potencies as inhibitors of selected recombinant human carbonic anhydrase (hCA) isozymes I, II, VII, and XIII were measured using isothermal titration calorimetry and the thermal shift assay. To determine the structural features of inhibitor binding, the crystal structures of several compounds in complex with hCA II were determined. Several compounds exhibited selectivity towards isozymes I, II, and XIII, and some were potent inhibitors of hCA VII.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Acetazolamide	Carbonic anhydrase 1	Kd (nM)	1400	N/A	N/A	Details
Acetazolamide	Carbonic anhydrase 1	Kd (nM)	780	N/A	N/A	Details
Acetazolamide	Carbonic anhydrase 2	Kd (nM)	17	N/A	N/A	Details
Acetazolamide	Carbonic anhydrase 2	Kd (nM)	18	N/A	N/A	Details