具有对碳酸酐酶同工酶I、II、IX和XII有效抑制活性的新型吖啶双磺酰胺的合成。
Synthesis of novel acridine bis-sulfonamides with effective inhibitory activity against the carbonic anhydrase isoforms I, II, IX and XII.
作者信息
Esirden İbrahim, Ulus Ramazan, Aday Burak, Tanç Muhammet, Supuran Claudiu T, Kaya Muharrem
机构信息
Chemistry Department, Faculty of Arts and Science, Dumlupınar University, 43100 Kütahya, Turkey.
Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche e Nutraceutiche, 50019 Sesto Fiorentino (Florence), Italy.
出版信息
Bioorg Med Chem. 2015 Oct 15;23(20):6573-80. doi: 10.1016/j.bmc.2015.09.022. Epub 2015 Sep 15.
By using a multi component reaction system (MCR), nitro acridine sulfonamides were obtained from cyclic-1,3-diketones, 4-aminobenzene sulfonamide and aromatic aldehydes. Some novel acridine bis-sulfonamides 6a-l were then synthesized by the reaction between sulfonyl chlorides and the novel amino-acridine sulfonamides 5a and 5b, obtained by reduction of nitro-acridine sulfonamide derivatives 4a and 4b. The newly synthesized compounds were investigated as inhibitors of 4 human carbonic anhydrase isoforms (hCA, EC 4.2.1.1). Several of the compounds showed low micromolar inhibition against the medically relevant isoforms hCA I, II, IX, and XII.
通过使用多组分反应体系（MCR），由环-1,3-二酮、4-氨基苯磺酰胺和芳香醛合成了硝基吖啶磺酰胺。然后，通过磺酰氯与通过还原硝基吖啶磺酰胺衍生物4a和4b得到的新型氨基吖啶磺酰胺5a和5b之间的反应，合成了一些新型吖啶双磺酰胺6a-l。对新合成的化合物作为4种人类碳酸酐酶同工型（hCA，EC 4.2.1.1）的抑制剂进行了研究。其中几种化合物对医学上相关的同工型hCA I、II、IX和XII表现出低微摩尔抑制作用。
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