Synthesis and antiviral evaluation of 1-O-hexadecylpropanediol-3-P-acyclovir: Efficacy against HSV-1 infection in mice
Synthesis and antiviral evaluation of 1-O-hexadecylpropanediol-3-P-acyclovir: Efficacy against HSV-1 infection in mice
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DOI：
10.1080/15257770008033022
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发表时间：
2000-01-01
影响因子：
1.3
通讯作者：
Hostetler, KY
中科院分区：
文献类型：
--
作者：
Beadle, JR;Kini, GD;Hostetler, KY
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-I 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.
