Synthesis and biological evaluation of lisofylline (LSF) analogs as a potential treatment for Type 1 diabetes

P Cui, TL Macdonald, M Chen, JL Nadler

Index: Cui, Peng; Macdonald, Timothy L.; Chen, Meng; Nadler, Jerry L. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 13 p. 3401 - 3405

Full Text: HTML

Citation Number: 32

Abstract

Lisofylline (LSF, 1-(5-R-hydroxyhexyl)-3, 7-dimethylxanthine) is an anti-inflammatory agent that protects β-cells from Th1 cytokine-induced dysfunction and reduces the onset of Type 1 diabetes in non-obese diabetic (NOD) mice. Due to its low potency, poor oral bioavailability, and short half-life, the widespread clinical utility of LSF may be limited. Our goal has been to develop new agents based on the LSF structural motif that resolve the potency and ...