Novel water-soluble prodrugs of acyclovir cleavable by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme

…, S Cabrera, S de Castro, C García-Aparicio…

文献索引：Diez-Torrubia, Alberto; Garcia-Aparicio, Carlos; Cabrera, Silvia; De Meester, Ingrid; Balzarini, Jan; Camarasa, Maria-Jose; Velazquez, Sonsoles Journal of Medicinal Chemistry, 2010 , vol. 53, # 2 p. 559 - 572

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被引用次数: 12

摘要

Abstract We herein report for the first time the successful use of the dipeptidyl peptidase IV (DPPIV/CD26) prodrug approach to guanine derivatives such as the antiviral acyclovir (ACV). The solution-and solid-phase synthesis of the tetrapeptide amide prodrug 3 and the tripeptide ester conjugate 4 of acyclovir are reported. The synthesis of the demanding tetrapeptide amide prodrug of ACV 3 was first established in solution and successfully ...