Premium
Synthesis of Novel Benzoic Acid Derivatives with Benzothiazolyl Subunit and Evaluation as Aldose Reductase Inhibitors
Author(s) -
Rakowitz Dietmar,
Hennig Barbara,
Nagano Marietta,
Steger Stefan,
Costantino Luca,
Matuszczak Barbara
Publication year - 2005
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200500101
Subject(s) - aldose reductase , chemistry , benzoic acid , stereochemistry , enzyme , derivative (finance) , aldose , protein subunit , chemical synthesis , biochemistry , combinatorial chemistry , glycoside , in vitro , financial economics , economics , gene
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.