二氟甲磺酰胺的新合成方法——一种用于碳酸酐酶抑制的新型药效基团。
A new synthesis of difluoromethanesulfonamides--a novel pharmacophore for carbonic anhydrase inhibition.
作者信息
Boyle Nicholas A, Chegwidden W Richard, Blackburn G Michael
机构信息
Krebs Institute, Chemistry Department, Sheffield University, Sheffield, UK S3 7HF.
出版信息
Org Biomol Chem. 2005 Jan 21;3(2):222-4. doi: 10.1039/b416642f. Epub 2004 Dec 15.
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.
关键中间体羧基二氟甲磺酰胺的制备为多种新型二氟甲磺酰胺提供了直接的合成途径，包括乙酰唑胺类似物（2-乙酰氨基-1,3,4-噻二唑-5-基）-二氟甲磺酰胺。它们的水溶性和稳定性、醚分配系数、pK(a)以及对人碳酸酐酶同工酶II（HCA II）的亚微摩尔解离常数使其成为局部青光眼治疗的有前景的候选药物。
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