Synthesis and antiviral activity of water-soluble esters of acyclovir [9-[(2-hydroxyethoxy) methyl] guanine)

L Colla, E De Clercq, R Busson…

Index: Colla, Leon; Clercq, Erik De; Busson, Roger; Vanderhaeghe, Hubert Journal of Medicinal Chemistry, 1983 , vol. 26, # 4 p. 602 - 604

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Citation Number: 123

Abstract

Several water-soluble ester derivatives of acyclovir [9-[(2-hydroxyethoxy) methyl] guanine], ie, the 2'-O-glycyl-, 2'-0-a-alanyl-, Z'-O-fi-alanyl-and 2'-0-3-carboxypropionyl esters, were synthesized and evaluated for their antiviral activity in cell culture. The compounds were all prepared directly from acyclovir by application of the usual esterification methods with the appropriate acyl precursors and isolated as their hydrochloride or sodium salts. When ...