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II. MEDICINAL CHEMISTRY OF NUCLEOSIDES/NUCLEOTIDES

Structure-Activity Relationship of Pyrimidine Heterosubstituted Nucleoside Analogues

, , , , , , & show all
Pages 993-1001 | Published online: 16 Aug 2006
 

Abstract

The structure-activity relationship of sixteen 3-deaza, C-4 substituted pyrimidines and imidazo[1,2-c]pyrimidine bases of 1,3-oxathiolanes and 1,3-dioxolanes revealed good anti-HBV activity in 2.2.15 cells transfected with human hepatitis B virus of the imidazo[1,2-c]pyrimidine nucleosides 21, 25 and 29. Two procedures for the preparation of C-4 substituted analogues are reported based on nucleophilic displacement of a sulfonamide or imidazole by a variety of nitrogen nucleophiles.

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