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Design synthesis and evaluation of novel aldose reductase inhibitors: The case of indolyl-sulfonyl-phenols.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2020 Aug 01; Vol. 28 (15), pp. 115575. Date of Electronic Publication: 2020 Jun 04. - Publication Year :
- 2020
-
Abstract
- Therapeutic interventions with aldose reductase inhibitors appear to be a promising approach to major pathological conditions (i.e. neuropathy/angiopathy related to chronic hyperglycemia, chronic inflammation and cancer). Until now, the most potent aldose reductase inhibitors have been carboxylic acid derivatives, which poorly permeate biological membranes. In this work, continuing our previous works, we promote the bioisosteric replacement of the carboxylic acid moiety to make equally potent yet more druggable inhibitors.<br /> (Copyright © 2020 Elsevier Ltd. All rights reserved.)
- Subjects :
- Aldehyde Reductase chemistry
Aldehyde Reductase metabolism
Animals
Catalytic Domain
Drug Design
Enzyme Assays
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors metabolism
Indoles chemical synthesis
Indoles metabolism
Molecular Docking Simulation
Phenols chemical synthesis
Phenols metabolism
Protein Binding
Rats
Sulfones chemical synthesis
Sulfones metabolism
Aldehyde Reductase antagonists & inhibitors
Enzyme Inhibitors chemistry
Indoles chemistry
Phenols chemistry
Sulfones chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 28
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 32631572
- Full Text :
- https://doi.org/10.1016/j.bmc.2020.115575