Synthesis and Biological Evaluations as Inhibitors of Human Parainfluenza Virus-1 based on the Computational Design for Prevention of Multi-infectious Diseases
| 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
|
| Project Status |
Completed (Fiscal Year 2014)
|
| 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)
|
|---|
| 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.
|
Report
(4 results)
Research Products
(31 results)
-
-
-
-
-
[Journal Article] Visualization of sialidase activity in mammalian tissues and cancer detection with a novel fluorescent sialidase substrate2014
Author(s)
Akira Minami1, Tadamune Otsubo, Daisuke Ieno, Kiyoshi Ikeda, Hiroaki Kanazawa, Kosuke Shimizu,Ko Ohata, Tsunehiro Yokochi, Yuuki Horii1, Hokuto Fukumoto1, Risa Taguchi1, Tadanobu Takahashi1,Naoto Oku, Takashi Suzuki
-
Journal Title
Related Report
Peer Reviewed / Acknowledgement Compliant
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
