Phosphoramidate derivatives of 2′,3′-didehydro-2′,3′-dideoxyadenosine [d4A] have markedly improved anti-HIV potency and selectivity

New 5′-phosphate derivatives of the nucleoside analogue d4A were prepared as potential membrane-soluble prodrugs of the free nucleotide. The anti-viral potency and selectivity of the derivatiyes is markedly increased by comparison to the parent nucleoside analogue. The new analogues show particular promise for further pre-clinical development.