Premium
On the Synthesis of Bioisosters of O ‐Benzothiazolyloxybenzoic Acids and Evaluation as Aldose Reductase Inhibitors
Author(s) -
Rakowitz Dietmar,
Muigg Patric,
Schröder Nicole,
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.200500119
Subject(s) - aldose reductase , chemistry , oxime , aldehyde reductase , substituent , bioisostere , stereochemistry , aldose reductase inhibitor , chemical synthesis , enzyme , enzyme inhibitor , biochemistry , in vitro
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.