Synthesis of novel benzoic acid derivatives with benzothiazolyl subunit and evaluation as aldose reductase inhibitors

被引:18
作者
Rakowitz, D
Hennig, B
Nagano, M
Steger, S
Costantino, L
Matuszczak, B
机构
[1] Univ Innsbruck, Inst Pharm, A-6020 Innsbruck, Austria
[2] Univ Modena, Dipartimento Sci Farmaceut, I-41100 Modena, Italy
关键词
methyl benzothiazolyloxybenzoates; benzothiazolyloxybenzoic acids; aldose reductase inhibitors; diabetic complications;
D O I
10.1002/ardp.200500101
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several methyl benzothiazolyloxybenzoates, S-isosters, and the corresponding benzoic acids were synthesized and tested as aldose reductase inhibitors (ARIs). Out of this series, the ester derivative 2a-7 was found to exhibit the highest enzyme-inhibitoric activity. In order to investigate this unexpected result, further modifications were carried out which allowed us to explain this finding and to open a path to a novel class of ARIs.
引用
收藏
页码:411 / 418
页数:8
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