title: 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.
abstract: 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 using Schistosoma mansoni worm 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.
authors.affiliation: Department of Pharmacology, Theodor Bilharz Research Institute, Warrak el-Hadar, Imbaba, Giza, Egypt.
authors.forename: Sanaa S
authors.initials: SS
authors.lastname: Botros
authors.forename: Samia
authors.initials: S
authors.lastname: William
authors.forename: James R
authors.initials: JR
authors.lastname: Beadle
authors.forename: Nadejda
authors.initials: N
authors.lastname: Valiaeva
authors.forename: Karl Y
authors.initials: KY
authors.lastname: Hostetler
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D006224:Cricetinae; D008647:Mesocricetus; D015394:Molecular Structure; D063065:Organophosphonates / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D012547:Schistosoma / Q000187:drug effects*; D012552:Schistosomiasis / Q000188:drug therapy* / Q000469:parasitology; D012556:Schistosomicides / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use*
chemical_list: D063065:Organophosphonates; D012556:Schistosomicides; C050127:9-(S)-(3-hydroxy-2-(phosphonomethoxy)propyl)adenine; D000225:Adenine
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