A new synthesis of difluoromethanesulfonamides - a novel pharmacophore for carbonic anhydrase inhibition

被引：13

作者：

Boyle, NA

Chegwidden, WR

Blackburn, GM ^{[1
]}

机构：

[1] Univ Sheffield, Krebs Inst, Dept Chem, Sheffield S3 7HF, S Yorkshire, England

[2] Sheffield Hallam Univ, Sheffield S1 1WB, S Yorkshire, England

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2005年 / 3卷 / 02期

关键词：

D O I：

10.1039/b416642f

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Preparation of the key intermediate carboxydifluoromethanesulfonamide provides direct synthetic access to a wide range of novel difluoromethanesulfonamides, including the acetazolamide analogue (2-ethanoylamino-1,3,4-thiadiazol- 5-yl)-difluoromethanesulfonamide. Their water solubility and stability, ether partition coefficient, pK(a) and submicromolar dissociation constants for human carbonic anhydrase isozyme II (HCA II) make them promising candidates for topical glaucoma therapy.

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页码：222 / 224

页数：3

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