Novel Inhibitors of Advanced Glycation Endproducts

Enhanced formation and accumulation of advanced glycation endproducts (AGE's) have been proposed to play a major role in the pathogenesis of diabetic complications, aging, atherosclerosis, and Alzheimer disease leading to progressive and irreversible intermolecular protein crosslinkings. This p...

Full description

Saved in:
Bibliographic Details
Published in:Biochemical and biophysical research communications 1999-09, Vol.262 (3), p.651-656
Main Authors: Rahbar, Samuel, Kumar Yernini, Kiran, Scott, Stephen, Gonzales, Noe, Lalezari, Iraj
Format: Article
Language:English
Subjects:
Animals
Antibodies
Butyrates - chemical synthesis
Butyrates - chemistry
Butyrates - pharmacology
Dipeptides - chemistry
Female
Glycated Hemoglobin A - drug effects
Glycation End Products, Advanced - antagonists & inhibitors
Humans
Indicators and Reagents
Rabbits
Ribonucleases - chemistry
Ribonucleases - drug effects
Ribose
Serum Albumin - drug effects
Structure-Activity Relationship
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Enhanced formation and accumulation of advanced glycation endproducts (AGE's) have been proposed to play a major role in the pathogenesis of diabetic complications, aging, atherosclerosis, and Alzheimer disease leading to progressive and irreversible intermolecular protein crosslinkings. This process is accelerated in diabetes and has been postulated to contribute to the development of a range of diabetic complications including nephropathy, retinopathy and neuropathy. Several potential drug candidates as AGE inhibitors have been reported recently. Aminoguanidine is the first drug extensively studied both in vitro and in vivo. We have developed a new class of compounds as potent inhibitors of glycation and AGE formation. The novel inhibitors reported here are aryl (and heterocyclic) ureido, and aryl (and heterocyclic) carboxamido phenoxy isobutyric acids and related molecules, which were found by in vitro assay methods to be potent inhibitors of multiple stage of glycation and AGE formation.
ISSN:0006-291X
1090-2104
DOI:10.1006/bbrc.1999.1275