A facile synthesis and anti-avian influenza virus (H5N1) screening of some novel pyrazolopyrimidine nucleoside derivatives |
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Authors: | Rashad Aymn E Shamroukh Ahmed H Abdel-Megeid Randa E Mostafa Ahmed Ali Mohamed A Banert Klaus |
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Institution: | Photochemistry Department, National Research Center, Elbehos Street, Dokki, Cairo, Egypt. aymnelzeny@yahoo.com |
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Abstract: | Treatment of 5-amino-1-(9-methyl-5,6-dihydronaphtho1',2':4,5]thieno2,3-d]pyrimidin-11-yl)-1H-pyrazole-4-carbonitrile (1) with formic acid afforded pyrazolo3,4-d]pyrimidin-4-one derivative 2. The sodium salt of the latter compound (generated in situ) was treated with some alkyl halides to afford the corresponding N-substituted compounds 3-7. The siloxy derivative 8 (generated also in situ from 2) was ribosylated and glycosylated to yield compounds 9 and 11, respectively. Deprotection of compounds 9 and 11 in methanolic ammonia produced the free nucleosides 10 and 12, respectively. Moreover, the prepared compounds were tested for antiviral activity against H5N1 virus A/chicken/Egypt/1/2006] and some of them revealed moderate results compared with the other tested compounds. |
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