ChemInform Abstract: Synthesis and Antiviral Evaluation of 1-O-Hexadecylpropanediol-3-P-acyclovir: Efficacy Against HSV-1 Infection in Mice

Autor:	Ganesh D. Kini, Kathy A. Aldern, Kristine N. Wright, Rachel J. Rybak, Earl R. Kern, Michael F. Gardner, Karl Y. Hostetler, James R. Beadle
Rok vydání:	2010
Předmět:	Chemistry viruses virus diseases General Medicine HSL and HSV biochemical phenomena metabolism and nutrition Prodrug medicine.disease_cause Virology In vitro Herpes simplex virus In vivo Thymidine kinase 1-O-hexadecylpropanediol-3-p-acyclovir medicine Nucleic acid heterocyclic compounds
Zdroj:	ChemInform. 31
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200029200
Popis:	We synthesized, 1-O-hexadecylpropanediol-3–P-acyclovir, an orally bioavailable lipid prodrug of acyclovir and evaluated it for in vitro and in vivo activity against herpes simplex virus infections. Although 1-O-hexadecylpropanediol-3–P-acyclovir was less active in vitro than acyclovir, on a molar basis it was 2.4 times more active orally in preventing mortality from acute HSV-1 infection in mice. In vitro, 1–O-hexadecylpropanediol-3–P-acyclovir was also more active than acyclovir in a thymidine kinase negative mutant strain of HSV-1 (DM21) and had somewhat higher activity in cytomegalovirus infection in vitro due to it's ability to bypass thymidine kinase.
Databáze:	OpenAIRE
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