Adamantane as a brain??directed drug carrier for poorly absorbed drug. 2. AZT derivatives conjugated with the 1??adamantane moiety

N Tsuzuki, T Hama, M Kawada, A Hasui…

Index: Tsuzuki; Hama; Kawada; Hasui; Konishi; Shiwa; Ochi; Futaki; Kitagawa Journal of Pharmaceutical Sciences, 1994 , vol. 83, # 4 p. 481 - 484

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Citation Number: 68

Abstract

Abstract Five AZT (azidothymidine) prodrugs conjugated with the 1-adamantane moiety via an ester bond were synthesized to improve the transport of AZT into the central nervous system (CNS). In in vitro degradation studies with rat and human plasma, it was demonstrated that the prodrugs were degradated enzymatically and converted quantitatively to their parent drug, AZT. As assessed by octanol–buffer partitioning, the prodrugs were ...