Synthesis and antiviral activity of the carbocyclic analogues of (E)-5-(2-halovinyl)-2'-deoxyuridines and (E)-5-(2-halovinyl)-2'-deoxycytidines

作者: Piet Herdewijn , Erik De Clercq , Jan Balzarini , Hubert Vanderhaeghe

DOI: 10.1021/JM50001A003

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摘要: The carbocyclic analogues of the potent and selective antiherpes agents (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU), (E)-5-(2-iodovinyl)-2'-deoxyuridine (IVDU), (E)-5-(2-bromovinyl)-2'-deoxycytidine (BVDC) were synthesized by conventional methods with use 2'-deoxyuridine as starting material. C-BVDU, C-IVDU, C-BVDC equally selective, albeit slightly less potent, in their action than BVDU, IVDU, BVDC. Although resistant to degradation pyrimidine nucleoside phosphorylases, C-BVDU did not prove more effective BVDU systemic (oral, intraperitoneal) or topical treatment HSV-1 infections mice.

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