Simple mono-derivatisation of the aryl moiety of D4A and DDA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture.
作者信息
Siddiqui A Q, McGuigan C, Ballatore C, Wedgwood O, De Clercq E, Balzarini J
机构信息
Welsh School of Pharmacy, Cardiff University, UK.
出版信息
Bioorg Med Chem Lett. 1999 Sep 6;9(17):2555-60. doi: 10.1016/s0960-894x(99)00416-3.
Abstract
Simple mono-derivatisation of the aryl moiety of some phosphoramidate pronucleotide derivatives of d4A and ddA served to increase the lipophilicity of these membrane-soluble prodrugs. A concomitant and significant enhancement of potency against HIV-1 and HIV-2 in vitro was observed for the ddA- and d4A-based prodrugs compared to the original underivatised prodrugs.
摘要
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