| Budget Amount *help |
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2014: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
|
|---|
| 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.
|
