title: Inhibition and breaking of advanced glycation end-products (AGEs) with bis-2-aminoimidazole derivatives.
abstract: Advanced glycation end-products (AGEs), unregulated modifications to host macromolecules that occur as a result of metabolic dysregulation, play a role in many diabetes related complications, inflammation and aging, and may lead to increased cardiovascular risk. Small molecules that have the ability to inhibit AGE formation, and even break preformed AGEs have enormous therapeutic potential in the treatment of these disease states. We report the screening of a series of 2-aminoimidazloles for anti-AGE activity, and the identification of a bis-2-aminoimidazole lead compound that possesses superior AGE inhibition and breaking activity compared to the known AGE inhibitor aminoguanidine.
authors.affiliation: Department of Microbiology, Immunology and Pathology, Mycobacteria Research Laboratories, Colorado State University, Forth Collins, CO 80524, USA.
authors.forename: Mike A
authors.initials: MA
authors.lastname: Richardson
authors.affiliation: Department of Chemistry, North Carolina State University, Raleigh, NC 27695, USA.
authors.forename: Robert E
authors.initials: RE
authors.lastname: Furlani
authors.affiliation: Department of Microbiology, Immunology and Pathology, Mycobacteria Research Laboratories, Colorado State University, Forth Collins, CO 80524, USA.
authors.forename: Brendan K
authors.initials: BK
authors.lastname: Podell
authors.affiliation: Department of Microbiology, Immunology and Pathology, Mycobacteria Research Laboratories, Colorado State University, Forth Collins, CO 80524, USA.
authors.forename: David F
authors.initials: DF
authors.lastname: Ackart
authors.affiliation: Department of Microbiology, Immunology and Pathology, Mycobacteria Research Laboratories, Colorado State University, Forth Collins, CO 80524, USA.
authors.forename: Jessica D
authors.initials: JD
authors.lastname: Haugen
authors.affiliation: Department of Chemistry, North Carolina State University, Raleigh, NC 27695, USA.
authors.forename: Roberta J
authors.initials: RJ
authors.lastname: Melander
authors.affiliation: Department of Chemistry, North Carolina State University, Raleigh, NC 27695, USA.
authors.forename: Christian
authors.initials: C
authors.lastname: Melander
authors.affiliation: Department of Microbiology, Immunology and Pathology, Mycobacteria Research Laboratories, Colorado State University, Forth Collins, CO 80524, USA.
authors.forename: Randall J
authors.initials: RJ
authors.lastname: Basaraba
keywords: Advanced glycation end-products (AGEs); Aminoguanidine; Bis-2-aminoimidazole; Diabetes