| Budget Amount *help |
¥3,100,000 (Direct Cost: ¥3,100,000)
Fiscal Year 1998: ¥400,000 (Direct Cost: ¥400,000)
Fiscal Year 1997: ¥2,700,000 (Direct Cost: ¥2,700,000)
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| Research Abstract |
The fusion peptide, which has been composed of 20 hydrophobic amino acids, exists in the surface of the virus and has important role in the adsorption and fusion to the host cell.
In this study, the bioactive protecting group unit was used within this amino acid sequence at the N-terminus tripeptide.
First, fusion peptide analogue of a RS virus having the Z (benzyloxycarbonyl) -tripeptide (Z-FLG) was synthesized by usual manner and this tripeptide showed the antiviral activity against RS virus.
In addition, the protecting group with the resistant antiviral activity was searched.
As well as usual medical supply development, when phenoxyacetyl unit of the length equal to the Z- group was used considering the molecular length, the activity lowered a little.
Next, the activity was not completely shown in phenylpropionyl unit which changed oxygen atom to carbon atom, having the same length with Z-group, in mandelyl unit which shifted the oxygen atom from the carbon skeleton chain, and in phenylacetyl unit except for the oxygen atom besides.
In the Z unit substituted p-position of benzene ring with the nitro group of the electronwithdrawing, the expected activity was not shown. In trifluoroacetyl group of which the electronwithdrawing was the strongest, the activity was not completely shown.
Sulfonic acid derivatives are reported in great numbers in the result of having the antiviral activity against HIV, The amino acid with the N-acetylsulfanilyl group was synthesized, and next, the acetylamino unit was modified chemically.
The free amino group was diazotized, after the acetylamino unit of N-acetylsulfanilyl amino acid was hydrolyzed, and it was made to react with the active methylene compounds to afford the corresponding hydrazino compouds.
The hydrazino compounds obtained from the reaction of coumarin, which were relatively good yields, were converted into the dipeptide by meanes of active ester method. However, these dipeptides were not shown antiviral activity.
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