Prodrugs of 2′, 3′??didehydro??3′??deoxythymidine (D4T): Synthesis, antiviral activity, and rapid pharmacokinetic evaluation

DR Tortolani, JW Russell, VJ Whiterock…

文献索引：Tortolani; Russell; Whiterock; Hitchcock; Ghazzouli; Martin; Mansuri; Starrett Jr. Journal of Pharmaceutical Sciences, 1994 , vol. 83, # 3 p. 339 - 343

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被引用次数: 8

摘要

Abstract A series of 5′-derivatives and modified pyrimidine analogues of 2′, 3′- didehydro-3′-deoxythymidine (d4T, stavudine, 1) were synthesized to determine their potential as oral prodrugs of d4T. Utilizing a screen developed for the rapid evaluation of a variety of prodrugs in mice, it was determined that 5′-acetate 2 provided comparable plasma levels of d4T after oral administration of the prodrug to that when d4T was ...