Design, Synthesis, and Structure-Activity Relationship Study of Novel Neuro-Protecting Drugs Based on Natural Product Hybridization

2015 Fiscal Year Final Research Report

• Project/Area Number: 25460010
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Chemical pharmacy
• Research Institution: University of Toyama
• Principal Investigator: Matsuya Yuji 富山大学, 大学院医学薬学研究部(薬学), 教授 (50255858)
• Co-Investigator(Renkei-kenkyūsha): SUGIMOTO KENJI 富山大学, 大学院医学薬学研究部, 准教授 (60400264) ; TOHDA CHIHIRO 富山大学, 和漢医薬学総合研究所, 准教授 (10272931)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: ハイブリッド化 / 天然物 / 神経賦活作用 / カップリング反応

Outline of Final Research Achievements

Novel hybridization compounds between steroidal natural product "denosomin" and its potential molecular target receptor "vitamin D3" were designed for the purpose of development of novel neuro-protecting agent toward Alzheimer disease chemotherapy. The syntheses were achieved by means of convergent synthetic strategy using palladium-catalyzed coupling reactions. The synthesized hybrid compounds were subjected to assay for their neuro-protecting activity, and new derivatives showing more potent activity than positive control compound "denosomin" were discovered.

Free Research Field

有機化学