Abstract
A novel series of acyl selenoureido benzensulfonamides was evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against the human (h) isoforms hCA I, II, VII and IX, which are involved in a variety of diseases such as glaucoma, retinitis pigmentosa, epilepsy and tumors etc. These compounds showed excellent inhibitory activity for these isoforms, with several low nanomolar derivatives identified against all of them. Furthermore, the selenoureido group may provide an antioxidant activity to these enzyme inhibitors.
Keywords:
Acylseleno-urea; Carbonic anhydrase; Inhibitors; Metalloenzymes; Selenium.
Copyright © 2017 Elsevier Ltd. All rights reserved.
MeSH terms
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Antigens, Neoplasm / metabolism
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Carbonic Anhydrase I / antagonists & inhibitors
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Carbonic Anhydrase I / metabolism
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Carbonic Anhydrase II / antagonists & inhibitors
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Carbonic Anhydrase II / metabolism
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Carbonic Anhydrase IX / antagonists & inhibitors
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Carbonic Anhydrase IX / metabolism
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Carbonic Anhydrase Inhibitors / chemical synthesis
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Carbonic Anhydrase Inhibitors / chemistry
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Carbonic Anhydrase Inhibitors / pharmacology*
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Carbonic Anhydrases / metabolism
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Dose-Response Relationship, Drug
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Humans
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Molecular Structure
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Organoselenium Compounds / chemical synthesis
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Organoselenium Compounds / chemistry
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Organoselenium Compounds / pharmacology*
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
Substances
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Antigens, Neoplasm
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Carbonic Anhydrase Inhibitors
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Organoselenium Compounds
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Sulfonamides
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Carbonic Anhydrase I
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Carbonic Anhydrase II
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CA9 protein, human
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Carbonic Anhydrase IX
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Carbonic Anhydrases
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carbonic anhydrase VI