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

✍ Scribed by Dietmar Rakowitz; Patric Muigg; Nicole Schröder; Barbara Matuszczak


Publisher
John Wiley and Sons
Year
2005
Tongue
English
Weight
115 KB
Volume
338
Category
Article
ISSN
0365-6233

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✦ Synopsis


Abstract

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.


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✍ Simona Rapposelli; Frederico Da Settimo; Maria Digiacomo; Concettina La Motta; A 📂 Article 📅 2011 🏛 John Wiley and Sons ⚖ 62 KB 👁 1 views

## Abstract A series of the title spirocyclic benzopyran derivatives (XI) (12 examples) is synthesized, which all prove to be selective inhibitors of aldose reductase (ARL2).