Publication Database

Synthesis of anthelmintically active N-methylated amidoxime analogues of the cyclic octadepsipeptide PF1022A (2002)

Art

Zeitschriftenartikel / wissenschaftlicher Beitrag

Autoren

Jeschke, Peter

Harder, Achim

von Samson-Himmelstjerna, Georg (WE 13)

Etzel, Winfried

Gau, Wolfgang

Thielking, Gerhard

Bonse, Gerhard

Quelle

Pest management science

Bandzählung: 58

Heftzählung: 12

Seiten: 1205 – 1215

ISSN: 1526-498x

Sprache

Englisch

Verweise

Pubmed: 12476993

Kontakt

Institut für Parasitologie und Tropenveterinärmedizin

Robert-von-Ostertag-Str. 7-13
14163 Berlin
+49 30 838 62310
parasitologie@vetmed.fu-berlin.de

Abstract / Zusammenfassung

The N-methylated amidoxime analogues of the cyclic octadepsipeptide PF1022A represent novel derivatives with activity against Trichinella spiralis Owen and Nippostrongylus brasiliensis Lane in vitro and against parasitic nematodes in mice and sheep. Some of them show better activity against Hymenolepis nana Siebold, Heterakis spumosa Schneider and Heligmosomoides polygyrus Dujardin in mice than the natural product PF1022A. In particular an improved efficacy against Haemonchus contortus Rudolphi and Trichostrongylus colubriformis Giles in sheep compared to the potent cyclic octadepsipeptide PF1022A and its mono-thionated derivative has been observed. Here we report on a specific modification at the N-methyl amide linkage by using the mono-thionated PF1022A, resulting in novel anthelmintically active backbone analogues of PF 1022A.