A Facile Synthesis and Anti-Avian Influenza Virus (H5N1) Screening of Some Novel Pyrazolopyrimidine Nucleoside Derivatives |
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Authors: | Aymn E Rashad Ahmed H Shamroukh Randa E Abdel-Megeid Ahmed Mostafa Mohamed A Ali Klaus Banert |
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Institution: | 1. Photochemistry Department , National Research Center , Dokki, Cairo, Egypt;2. Virology Laboratory, Water Pollution Department , National Research Center , Dokki, Cairo, Egypt;3. Organic Chemistry , Chemnitz University of Technology , Chemnitz, Germany |
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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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Keywords: | Pyrazoles pyrazolopyrimidines nucleosides anti-avian influenza virus (H5N1) |
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