Prodrugs of 2′, 3′??didehydro??3′??deoxythymidine

…, K Juni, M Saneyoshi, T Kawaguchi

Index: Hasegawa; Seki; Juni; Saneyoshi; Kawaguchi Journal of Pharmaceutical Sciences, 1993 , vol. 82, # 12 p. 1232 - 1236

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Citation Number: 8

Abstract

Abstract Six ester prodrugs of 2′, 3′-didehydro-3′-deoxythymidine (D4T) were synthesized, and their physicochemical properties were evaluated. Marked differences were observed. All of the prodrugs were chemically stable within the pH range 2–7. Hydrolysis of these esters was observed in all cases for four rat enzyme systems (plasma, liver, duodenum, and kidney), with D4T being regenerated. D4T or the prodrug was ...