Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3-and 4-(hetero)arylisoxazol-5-amine scaffolds

Krasavin Mikhail; Korsakov Mikhail; Zvonaryova ZhannaSemyonychev EvgeniiTuccinardi TizianoKalinin StanislavTanc MuhammetSupuran Claudiu T.

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Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3-and 4-(hetero)arylisoxazol-5-amine scaffolds

机译：Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3-and 4-(hetero)arylisoxazol-5-amine scaffolds

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Three distinct series of isoxazole-based primary mono- and bis-sulfonamides have been synthesized via direct sulfochlorination, each of them delivering nanomolar inhibitors of human carbonic anhydrase. Certain pronounced SAR trends have been established and rationalized by in silico docking. These findings expand the structure-activity knowledge base for heterocycle-containing sulfonamide carbonic anhydrase inhibitors and further validate the power of direct electrophilic sulfochlorination as a means of introducing the pharmacophoric primary sulfonamide group into structurally diverse aromatic precursors. (C) 2017 Elsevier Ltd. All rights reserved.

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《Bioorganic and medicinal chemistry》 |2017年第6期|1914-1925|共12页
作者
Krasavin Mikhail; Korsakov Mikhail; Zvonaryova ZhannaSemyonychev EvgeniiTuccinardi TizianoKalinin StanislavTanc MuhammetSupuran Claudiu T.;
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作者单位

St Petersburg State Univ, Inst Chem & Translat Biomed, R-199034 St Petersburg, Russia;

Ushinsky Yaroslavl State Pedag Univ, Yaroslavl, Russia;

Univ Pisa, Dept Pharm, Via Bonanno 6, I-56126 Pisa, ItalyUniv Firenze, Neurofarba Dept, Florence, Italy;

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正文语种英语
中图分类药学;
关键词
Carbonic anhydrase inhibitors; Isoform selectivity; Zinc binding group; Primary sulfonamide; Aromatic sulfochlorination; Alternative binding mode;

Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3-and 4-(hetero)arylisoxazol-5-amine scaffolds

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