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Short Paper | Regular issue | Vol 87, No. 11, 2013, pp.2369-2384
Published online, 4th October, 2013
DOI: 10.3987/COM-13-12824
A New Method for Synthesis and Angiogenic Evaluation of Leteprinim Potassium and Its Novel Analogs

Norikazu Sakakibara, Ikuko Tsukamoto, Yohei Isono, Maki Takata, Ryoji Konishi, Yoshihisa Kato, and Tokumi Maruyama*

*Kagawa School of Pharmaceutical Sciences, Tokushima Bunri University, 1314-1 Shido, Sanuki City, Kagawa 769-2193, Japan


We developed a novel pathway for the successful synthesis of leteprinim potassium 1, which is one of the candidate substances for treating Alzheimer’s disease, and subsequently synthesized 4 types of corresponding novel derivatives 2–5 that have hypoxanthine or 2-chloro-6-aminopurine as the nucleobase. We then determined the angiogenic activity of these compounds by using human umbilical vein endothelial cells. Compounds 1–4 showed no angiogenic potencies judging from statistical analysis, student’s t-test.