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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.
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页码:411 / 418
页数:8
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