Synthesis and biological activity of aminoguanidine and diaminoguanidine analogues of the antidiabetic/antiobesity agent 3-guanidinopropionic acid

…, PD May, MD Meglasson, DD Robinson…

Index: Vaillancourt; Larsen; Tanis; Burr; Connell; Cudahy; Evans; Fisher; May; Meglasson; Robinson; Stevens; Tucker; Vidmar; Yu Journal of Medicinal Chemistry, 2001 , vol. 44, # 8 p. 1231 - 1248

Full Text: HTML

Citation Number: 39

Abstract

3-Guanidinopropionic acid (1) has been demonstrated both to improve insulin sensitivity and to promote weight loss selectively from adipose tissue in animal models of non-insulin- dependent diabetes mellitus (NIDDM). However, 1 has also been shown to be a substrate for both the creatine transporter and creatine kinase, leading to marked accumulation in muscle tissue as the corresponding N-phosphate. The corresponding aminoguanidine ...