- Synthesis and biological activity of a series of methylene-expanded oxetanocin nucleoside analogues
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A series of methylene-expanded oxetanocin nucleoside analogues, e.g. analogues of 2 and the known antiviral nucleosides AZT, FLT, and ddC (3) were prepared by a very direct route beginning with the readily available (S)-glycidol 4 and proceeding via the dihydrofuran-3-methanols 9a,b. Biological testing of these modified nucleosides indicates that they are non-cytotoxic compounds with generally weak antiviral activity. However, the guanosine analogue 2G showed pronounced activity vs. herpes simplex virus type 1 (HSV-1) in cell culture and was HSV-1-encoded thymidine kinase dependent. This compound is therefore an interesting new lead structure for the development of new anti-HSV agents.
- Jung, Michael E.,Toyota, Akemi,De Clercq, Erik,Balzarini, Jan
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p. 499 - 520
(2007/10/03)
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- Efficient synthesis of several methylene-expanded oxetanocin nucleoside analogues
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S-Glycidol 4 has been converted by a direct route via the dihydrofuran- 3-methanols 9ab into a series of methylene-expanded oxetanocin nucleoside analogues, e.g., analogues of the normal nucleosides 2 and the known antiviral nucleosides, AZT, FdT, and ddC, 3. (C) 2000 Elsevier Science Ltd.
- Jung, Michael E.,Toyota, Akemi
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p. 3577 - 3581
(2007/10/03)
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