Benzoxaborole as a new chemotype for carbonic anhydrase inhibition

被引:68
作者
Alterio, Vincenzo [1 ]
Cadoni, Roberta [2 ,3 ]
Esposito, Davide [1 ]
Vullo, Daniela [4 ]
Di Fiore, Anna [1 ]
Monti, Simona Maria [1 ]
Caporale, Andrea [1 ]
Ruvo, Menotti [1 ]
Sechi, Mario [3 ]
Dumy, Pascal [2 ]
Supuran, Claudiu T. [5 ]
De Simone, Giuseppina [1 ]
Winum, Jean-Yves [2 ]
机构
[1] CNR, Ist Biostrutture & Bioimagini, Naples, Italy
[2] Univ Montpellier, ENSCM, CNRS UMR5247, IBMM, Montpellier, France
[3] Univ Sassari, Dipartimento Chim & Farm, Sassari, Italy
[4] Univ Florence, Sesto Fiorentino, Polo Sci, Lab Chim Bioinorgan, Florence, Italy
[5] Univ Florence, Sesto Fiorentino, Sect Pharmaceut & Nutriceut Sci, Neurofarba Dept, Florence, Italy
关键词
ARYLBORONIC ACIDS; ANTIFUNGAL AGENT; BORONOPHTHALIDE; IDENTIFICATION; BORTEZOMIB;
D O I
10.1039/c6cc06399c
中图分类号
O6 [化学];
学科分类号
070301 [无机化学];
摘要
In this paper we report the synthesis of a series of benzoxaborole derivatives, their inhibition properties against some carbonic anhydrases (CAs), recognized as important drug targets, and the characterization of the binding mode of these molecules to the CA active site. Our data provide the first experimental evidence that benzoxaboroles can be efficiently used as CA inhibitors.
引用
收藏
页码:11983 / 11986
页数:4
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