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KMID : 0043320070300020131
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Archives of Pharmacal Research
2007 Volume.30 No. 2 p.131 ~ p.137
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Synthesis of Novel 2’-Methyl Carbovir Analogues as Potent Antiviral Agents
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Hong Joon-Hee
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Abstract
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In this study, the synthesis procedures of 2’-branched carbovir analogues were accomplished. The introduction of a methyl group in the requisite 2’-position was carried out by the addition of a carbonyl using isopropenyl magnesium bromide. The desired compound, cyclopentenol 10(β), was synthesized via ring-closing metathesis using a second-generation Grubbs’ catalyst. The nucleosidic bases (adenine, cytosine, thymine, uracil, 5-fluorouracil and 5-iodouracil) were efficiently coupled using a Pd (0) catalyst. When the synthesized compounds were examined for their activity against several viruses, including HIV-1, HSV-1, HSV-2 and HCMV, the 5-iodouracil analogue, 23, exhibited significant anti-HCMV activity.
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KEYWORD
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Branched nucleoside, Antiviral agent, Grignard reaction
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