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新型酰基硒脲基苯磺酰胺作为碳酸酐酶I、II、VII和IX抑制剂的合成

Synthesis of novel acyl selenoureido benzensulfonamides as carbonic anhydrase I, II, VII and IX inhibitors.

作者信息

Angeli Andrea, Carta Fabrizio, Bartolucci Gianluca, Supuran Claudiu T

机构信息

Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.

Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.

出版信息

Bioorg Med Chem. 2017 Jul 1;25(13):3567-3573. doi: 10.1016/j.bmc.2017.05.014. Epub 2017 May 9.

DOI:10.1016/j.bmc.2017.05.014
PMID:28522267
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.

摘要

评估了一系列新型的酰基硒脲基苯磺酰胺作为碳酸酐酶（CA，EC 4.2.1.1）抑制剂对人（h）同工型hCA I、II、VII和IX的抑制作用，这些同工型参与多种疾病，如青光眼、色素性视网膜炎、癫痫和肿瘤等。这些化合物对这些同工型表现出优异的抑制活性，鉴定出了几种对所有同工型均具有低纳摩尔级抑制活性的衍生物。此外，硒脲基可能为这些酶抑制剂提供抗氧化活性。

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