Structure-Activity Relationship of Pyrimidine Heterosubstituted Nucleoside Analogues |
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| Authors: | Tarek S Mansour Colleen A Evans M Arshad Siddiqui Marie Charron Boulos Zacharie Nghe Nguyen-Ba |
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| Institution: | BioChem Therapeutic Inc. , 275 Armand-Frappier Boulevard, Laval, Québec, Canada , H7V 4A7 |
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| Abstract: | Abstract The structure-activity relationship of sixteen 3-deaza, C-4 substituted pyrimidines and imidazo1,2-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 imidazo1,2-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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