On the Synthesis of Bioisosters of O-Benzothiazolyloxybenzoic Acids and Evaluation as Aldose Reductase Inhibitors

In continuation of our attempts to develop novel aldose reductase inhibitors (ARIs), a number of compounds characterized by bioisosteric replacement of pharmacophors were prepared. On the one hand, the acidic function was formally replaced by an oxime or a nitro group and on the other hand the lipop...

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Veröffentlicht in:Archiv der Pharmazie (Weinheim) 2005-09, Vol.338 (9), p.419-426
Hauptverfasser: Rakowitz, Dietmar, Muigg, Patric, Schröder, Nicole, Matuszczak, Barbara
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container_title Archiv der Pharmazie (Weinheim)
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creator Rakowitz, Dietmar
Muigg, Patric
Schröder, Nicole
Matuszczak, Barbara
description In continuation of our attempts to develop novel aldose reductase inhibitors (ARIs), a number of compounds characterized by bioisosteric replacement of pharmacophors were prepared. On the one hand, the acidic function was formally replaced by an oxime or a nitro group and on the other hand the lipophilic substituent was modified. The results of the biological evaluation of these derivatives enabled us to gain insight into structural features critical for the aldose reductase inhibition.
doi_str_mv 10.1002/ardp.200500119
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subjects Aldehyde Reductase - antagonists & inhibitors
Aldose reductase inhibitors
Animals
Benzoates - chemical synthesis
Benzoates - chemistry
Bioisosteric replacement
Biological and medical sciences
Cattle
Diabetic complications
Enzyme inhibitors
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
General and cellular metabolism. Vitamins
In Vitro Techniques
Lens, Crystalline - enzymology
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Structure-Activity Relationship
Thiazoles - chemical synthesis
Thiazoles - chemistry
title On the Synthesis of Bioisosters of O-Benzothiazolyloxybenzoic Acids and Evaluation as Aldose Reductase Inhibitors
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