The development of antidiabetic and antithrombogenic drugs using marine natural products as lead compounds

2014 Fiscal Year Final Research Report

• Project/Area Number: 24590145
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Showa University
• Principal Investigator: ITOH Takashi 昭和大学, 薬学部, 教授 (40159885)
• Co-Investigator(Kenkyū-buntansha): NAGATA Kazuhiro 昭和大学, 薬学部, 准教授 (20208010) ; KANEMITSU Takuya 昭和大学, 薬学部, 講師 (10372913)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: 不斉全合成 / α-グルコシダーゼ阻害薬 / 海洋天然物 / 抗血栓薬

Outline of Final Research Achievements

Schulzeine and Penasulfate, which are marine-derived natural products and have strong a-glucosidase inhibition activity, were synthesized using new synthetic methods developed by our group.　The bioactivity or these compounds were measured using a-glucosidase assay kit, and it was found that these are more active than commercially available a-glucosidase inhibitors. These compounds consist of a heterocyclic moiety and a long fatty acid moiety, and these are joined with an amide bond. Thus, the project was continued to synthesize hybridized compounds, which exchange the combination of these two parts.
In the synthesis of SMTP-7, we tried hard to complete the total synthesis, and found that a few more steps are necessary for the completion of the synthesis.

Free Research Field

有機合成化学