AI Article Synopsis
- The study focuses on the development of potent anti-HIV compounds based on specific analogues of beta-D-d4T.
- Initial findings indicated that an alkyl side-chain with 12 carbons was necessary for weak antiviral activity.
- The research progressed to creating phosphoramidate derivatives as potential prodrugs, but these new compounds showed no anti-HIV activity when tested.
Article Abstract
We have previously reported the synthesis and evaluation of potent anti-human immunodeficiency virus compounds based on beta-D-d4T analogues bearing a tether attached at the C-5 position and their beta-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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| http://dx.doi.org/10.1080/14756360500220343 | DOI Listing |
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