Synthesis and Biological Evaluations as Inhibitors of Human Parainfluenza Virus-1 based on the Computational Design for Prevention of Multi-infectious Diseases

2014 Fiscal Year Final Research Report

• Project/Area Number: 24590155
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Hiroshima International University
• Principal Investigator: IKEDA Kiyoshi 広島国際大学, 薬学部, 教授 (40168125)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: シアル酸 / パラインフルエンザウイルス / シアリダーゼ阻害剤

Outline of Final Research Achievements

Human parainfluenza virus type 1 (hPIV-1) is a serious pathogen causing upper and lower respiratory disease in infants and young children; however, there are no known effective inhibitors of hPIV-1 infection. We report herein the synthesis of 3,4-unsaturated sialic acid derivatives promoted by Bi(OTf)3-montmorillonite K-10 and their evaluation of their inhibitory activities against hPIV-1 sialidase. Among synthesized compounds, cyclohexyl derivative showed the most inhibitory activity against hPIV-1 sialidase (IC50 = 1.7 mM). However, the degree of its inhibition was much weaker than that of DANA (IC50 = 0.2 mM). It is suggested that the expression of inhibitory activity of sialic acid derivatives against hPIV-1 requires the structural feature of a 2,3-double bond of sialic acid. The present findings should provide useful information for the development of anti-human parainfluenza virus compounds.

Free Research Field

薬学・創薬化学・生物活性物質