期刊
ARCHIV DER PHARMAZIE
卷 355, 期 3, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.202100405
关键词
1; 2; 3-triazolo-benzodiazepines; 1; 5-benzodiazepin-2-ones; benzene sulfonamide; carbonic anhydrase inhibitors; CuAAC click chemistry
资金
- University of Montpellier
- ENSCM
- Ministry of Higher Education and Scientific Research of Tunisia
- IBMM
A series of novel N-triazole-benzene sulfonamides-1,5-benzodiazepines were designed and synthesized through copper-catalyzed click chemistry, with one compound showing high inhibitory activity against various isoforms of human carbonic anhydrase.
A series of novel N-triazolo-benzene sulfonamides-1,5-benzodiazepines 9a-d and 10d were designed and prepared through the copper-catalyzed azide alkyne cycloaddition click chemistry procedure, reacting the N-1-propargyl-1,5-benzodiazepine 2 and the N-1,N-5-dipropargyl analog 6 with various benzene sulfonamide azides 8a-d. The synthesized compounds were found to show nanomolar affinity toward relevant isoforms of human carbonic anhydrase such as hCA I, II, IV, VII, IX, and XII. The divalent derivative 10d showed a particularly high inhibitory activity against all hCA isoforms when compared with acetazolamide, and showed potent multivalent effects, better than reported previously for divalent CA inhibitors.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据