Author： Ladurée Daniel Fossey Christine Delbederi Zoica Sugeac Elena Schmidt Sylvie Laumond Geraldine Aubertin Anne-Marie
Publisher： Informa Healthcare
ISSN： 1475-6366
Source： Journal of Enzyme Inhibition and Medicinal Chemistry, Vol.20, Iss.6, 2005-12, pp. : 533-549
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Abstract
We have previously reported the synthesis and evaluation of potent anti-human immunodeficiency virus compounds based on β-D-d4T analogues bearing a tether attached at the C-5 position and their β-L-counterparts. Initial study revealed a requirement for an alkyl side-chain with an optimal length of 12 carbons for a weak antiviral activity. As a continuation of that work, we have now prepared the corresponding phosphoramidate derivatives as possible membrane-permeable prodrugs. Phosphorochloridate chemistry gave the target phosphoramidates which were tested for anti-human immunodeficiency virus type 1 activity; unfortunately, they were devoid of anti-HIV activity.
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