Synthesis and biological evaluation of 5-substituted derivatives of the potent antiherpes agent (north)-methanocarbathymine

P Russ, P Schelling, L Scapozza…

Index: Russ, Pamela; Schelling, Pierre; Scapozza, Leonardo; Folkers, Gerd; De Clercq, Erik; Marquez, Victor E. Journal of Medicinal Chemistry, 2003 , vol. 46, # 23 p. 5045 - 5054

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Citation Number: 61

Abstract

The conformationally locked nucleoside,(north)-methanocarbathymine (1a), is a potent and selective anti-herpes agent effective against herpes simplex type 1 (HSV1) and type 2 (HSV2) viruses. Hereby, we report on the synthesis and biological evaluation of a small set of 5-substituted pyrimidine nucleosides belonging to the same class of bicyclo [3.1. 0] hexane nucleosides. Both the 5-bromovinyl (4) and the 5-bromo analogue (3) appeared to ...