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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:25

Article

Furlani, Robert E.¹  Richardson, Mike A.²  Podell, Brendan K.²  Ackart, David F.²  Haugen, Jessica D.²  Melander, Roberta J.¹  Basaraba, Randall J.²  Melander, Christian¹ 

[1] N Carolina State Univ, Dept Chem, Raleigh, NC 27695 USA

[2] Colorado State Univ, Dept Microbiol Immunol & Pathol, Mycobacteria Res Labs, Ft Collins, CO 80524 USA

关键词: Advanced glycation end-product (AGE);    2-Aminoimidazole;    Akabori;    Diabetes;   

DOI  :  10.1016/j.bmcl.2015.06.080

来源: Elsevier

【 摘 要 】

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. (C) 2015 Elsevier Ltd. All rights reserved.

【 授权许可】

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