Second generation 2-aminoimidazole based advanced glycation end product inhibitors and breakers

作者：Furlani Robert E; Richardson Mike A; Podell Brendan K; Ackart David F; Haugen Jessica D; Melander Roberta J; Basaraba Randall J^*; Melander Christian

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(21): 4820-4823.

DOI：10.1016/j.bmcl.2015.06.080

• Advanced glycation end-product (AGE)
• 2-Aminoimidazole
• Akabori
• Diabetes

The formation of advanced glycation end-products (AGE) as a result of the action of reducing sugars on host macromolecules plays a role in increased morbidity of diabetic patients. There are currently no clinically available therapeutics for the prevention or eradication of AGEs. Following our previous identification of 2-aminoimidazole (2-AI) based AGE inhibitors and breakers, we now report the use of a rapid, scalable, two-step procedure to access a second generation of 2-AI based anti-AGE compounds from commercially available amino acids. Several second generation compounds exhibit increased AGE inhibition and breaking activty compared to the first generation compounds and to the known AGE inhibitor aminoguanidine.

• 出版日期2015-11-1