Synthesis of anthelmintically activeN-methylated amidoxime analogues of the cyclic octadepsipeptide PF1022A
| Autor: | Achim Harder, Gerhard Thielking, Winfried Etzel, Peter Jeschke, Gerhard Bonse, Georg von Samson-Himmelstjerna, Wolfgang Gau |
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| Rok vydání: | 2002 |
| Předmět: |
Hymenolepis nana
Magnetic Resonance Spectroscopy Nematoda Trichostrongylus Stereochemistry Trichinella Trichinella spiralis Peptides Cyclic Mice Structure-Activity Relationship Depsipeptides Oximes parasitic diseases medicine Animals Anthelmintic Nippostrongylus brasiliensis Anthelmintics Depsipeptide Nematospiroides dubius Sheep biology Biological activity General Medicine biology.organism_classification Models Chemical Insect Science Immunology Haemonchus Nippostrongylus Heligmosomoides polygyrus Helminthiasis Animal Agronomy and Crop Science Hymenolepis medicine.drug Haemonchus contortus |
| Zdroj: | Pest Management Science. 58:1205-1215 |
| ISSN: | 1526-4998 1526-498X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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