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N-酰基磺胺类化合物:药物化学中的合成路线及生物学潜力

N-acylsulfonamides: Synthetic routes and biological potential in medicinal chemistry.

作者信息

Ammazzalorso Alessandra, De Filippis Barbara, Giampietro Letizia, Amoroso Rosa

机构信息

Dipartimento di Farmacia, Università G. d'Annunzio, Chieti, Italy.

出版信息

Chem Biol Drug Des. 2017 Dec;90(6):1094-1105. doi: 10.1111/cbdd.13043. Epub 2017 Jul 11.

Abstract

Sulfonamide is a common structural motif in naturally occurring and synthetic medicinal compounds. The rising interest in sulfonamides and N-acyl derivatives is attested by the large number of drugs and lead compounds identified in last years, explored in different fields of medicinal chemistry and showing biological activity. Many acylsulfonamide derivatives were designed and synthesized as isosteres of carboxylic acids, being the characteristics of these functional groups very close. Starting from chemical routes to N-acylsulfonamides, this review explores compounds of pharmaceutical interest, developed as enzymatic inhibitors or targeting receptors.

摘要

磺胺是天然存在和合成药物化合物中常见的结构基序。近年来发现的大量药物和先导化合物在药物化学的不同领域进行了探索并显示出生物活性,这证明了人们对磺胺及其N-酰基衍生物的兴趣日益浓厚。许多酰基磺胺衍生物被设计和合成作为羧酸的电子等排体,因为这些官能团的特性非常相似。从合成N-酰基磺胺的化学路线出发,本综述探讨了具有药物活性的化合物,这些化合物被开发为酶抑制剂或靶向受体。

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