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| - Does the Anti-Hepatitis B Virus Activity of (+)-5‘-Noraristeromycin Exist in Its4‘-Epimer and 4‘-Deoxygenated Derivatives?
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| - To begin an exploration of the structural parametersresponsible for the activity of (+)-5‘-noraristeromycin toward hepatitis B virus (HBV), three derivativesvaried at the C-4‘ positionhave been prepared and evaluated. The syntheses began with aMitsunobu coupling reactionof an appropriate cyclopentanol with 6-chloropurine. The productsof these reactions weresynthetically altered by standard ammonolysis and deprotectionprocedures to give the desiredproducts. Evaluation of the new derivatives indicated that removalof the C-4‘ hydroxyl of(+)-5‘-noraristeromycin increased its potency toward HBV byapproximately 10-fold.
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