Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
复制标题
通过体外杀血吸虫评估十六烷氧基丙基环状 9-(S)-[3-羟基-2-(膦酰甲氧基)丙基]腺嘌呤和其他无环核苷膦酸酯的烷氧基烷基酯的抗血吸虫活性。
DOI：
10.1128/aac.00840-09
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发表时间：
2009
影响因子：
4.9
通讯作者：
Hostetler,KarlY
中科院分区：
文献类型：
--
作者：
Botros,SanaaS;William,Samia;Beadle,JamesR;Valiaeva,Nadejda;Hostetler,KarlY
已报告9-（S）-[3-羟基-2-（膦酰甲氧基）丙基]腺嘌呤[（S）-HPMPA]具有抗溶酶体活性。（S）-HPMPA和西多福韦（CDV）的醚脂质酯在抗病毒测定和痘病毒疾病的致死动物模型中具有大大增加的活性。为了观察CDV和（S）-HPMPA的醚脂酯是否增强抗溶酶体活性，我们在体外使用曼氏血吸虫杀灭试验了它们的烷氧基烷基酯。十六烷氧基丙基（HDP）-环-（S）-HPMPA和HDP-环-CDV表现出显着的体外抗溶酶体活性，并可能提供单独或与吡喹酮联合使用的前景。
9-(S)-[3-Hydroxy-2-(phosphonomethoxy)propyl]adenine [(S)-HPMPA] has been reported to have antischistosomal activity. Ether lipid esters of (S)-HPMPA and cidofovir (CDV) have greatly increased activities in antiviral assays and in lethal animal models of poxvirus diseases. To see if ether lipid esters of CDV and (S)-HPMPA enhance antischistosomal activity, we tested their alkoxyalkyl esters usingSchistosoma mansoniworm killing in vitro. Hexadecyloxypropyl (HDP)-cyclic-(S)-HPMPA and HDP-cyclic-CDV exhibited significant in vitro antischistosomal activities and may offer promise alone or in combination with praziquantel.