关键词: Aldose reductase Bioisosterism Indolyl–sulfonyl–phenols Inflammatory pathologies Long-term diabetic complications

Mesh : Aldehyde Reductase / antagonists & inhibitors chemistry metabolism Animals Catalytic Domain Drug Design Enzyme Assays Enzyme Inhibitors / chemical synthesis chemistry metabolism Indoles / chemical synthesis chemistry metabolism Molecular Docking Simulation Phenols / chemical synthesis chemistry metabolism Protein Binding Rats Sulfones / chemical synthesis chemistry metabolism

来  源:   DOI:10.1016/j.bmc.2020.115575   PDF(Sci-hub)

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.
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