Bioscience Biotechnology and Biochemistry · 2011 · 16 citations · 13 references
Veterinary MedicineEntomologyPharmacologyComparative PharmacologyDrug DiscoveryStructure-activity RelationshipsAnthelmintic PharmacologyAnthelmintic ResistanceAntiparasitic AgentsAntiparasitic PharmacologyNematode BiologyAnthelmintic AgentsAnthelmintic Drug ClassesAnthelmintic Drug DiscoveryMechanisms Of Anthelmintic ActionNematocidal ActivityStereochemical Structure - Activity RelationshipVeterinary Anthelmintics
The relationship between cyclooctadepsipeptides and their anthelmintic efficacy was examined by converting the natural products, PF1022A, PF1022E and PF1022H. Some analogues substituted at the para position of the phenyllactate moiety showed higher or equivalent activity against the parasitic nematode, Ascaridia galli in chicken when compared with the parent compounds. It is suggested that lipophilicity and the polar surface area, in addition to structural requirements of the derivatives, influenced the anthelmintic efficacy in vivo.
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