Synthesis and biological activity of analogues of the antidiabetic/antiobesity agent 3-guanidinopropionic acid: discovery of a novel aminoguanidinoacetic acid …

…, PD May, MD Meglasson, TJ O'Sullivan…

Index: Larsen; Connell; Cudahy; Evans; May; Meglasson; O'Sullivan; Schostarez; Sih; Stevens; Tanis; Tegley; Tucker; Vaillancourt; Vidmar; Watt; Yu Journal of Medicinal Chemistry, 2001 , vol. 44, # 8 p. 1217 - 1230

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Citation Number: 52

Abstract

3-Guanidinopropionic acid (1, PNU-10483) has been demonstrated to both 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 4. In an effort to identify ...