C. Meier et al., ADA-BYPASS BY LIPOPHILIC CYCLOSAL-DDAMP PRO-NUCLEOTIDES A 2ND EXAMPLEOF THE EFFICIENCY OF THE CYCLOSAL-CONCEPT, Bioorganic & medicinal chemistry letters, 7(12), 1997, pp. 1577-1582
The synthesis of lipophilic pro-nucleotides of ddAMP 2 based on cycloS
al-ddAMP 3a-c is described. Phosphotriesters 3 released ddAMP 2 select
ively by a controlled, chemically induced tandem reaction. CycloSal-ph
osphotriesters 3 exhibited antiviral activity against HIV-1/HIV-2 in C
EM cells that where by a factor up to hundred higher as compared to dd
A 1. (C) 1997 Elsevier Science Ltd.