title: Azadepsipeptides: synthesis and evaluation of a novel class of peptidomimetics.
abstract: A general route to azadepsipeptides, a new class of pseudopeptides, has been established. The methodology was applied to the synthesis of a bis-aza analogue of the antiparasitic cyclooctadepsipeptide PF1022A. Comparison of the X-ray crystal structures of natural PF1022A (8) and the chimeric aza analogue 9 revealed that the introduction of nitrogen in the backbone of PF1022A results in almost complete conservation of the 3D structure with only minor deviations at the new nitrogen positions.
authors.affiliation: Central Research and Business Group Animal Health, Bayer AG, D-51368 Leverkusen, Germany.
authors.forename: H
authors.initials: H
authors.lastname: Dyker
authors.forename: J
authors.initials: J
authors.lastname: Scherkenbeck
authors.forename: D
authors.initials: D
authors.lastname: Gondol
authors.forename: A
authors.initials: A
authors.lastname: Goehrt
authors.forename: A
authors.initials: A
authors.lastname: Harder
mesh_terms: D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D018360:Crystallography, X-Ray; D047630:Depsipeptides; D006188:Haemonchiasis / Q000188:drug therapy / Q000469:parasitology; D006189:Haemonchus; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D012756:Sheep; D014253:Trichostrongylosis / Q000188:drug therapy / Q000469:parasitology; D014254:Trichostrongylus
chemical_list: D000871:Anthelmintics; D047630:Depsipeptides; D007202:Indicators and Reagents; D009842:Oligopeptides; D010456:Peptides, Cyclic; C075544:PF 1022A