The cyclooctadepsipeptide PF1022A (1) and its semisynthetic, commercial
analogue emodepside (2) have been established as excellent anthelmintics with
resistance breaking properties. For a second generation anthelmintic cyclooctadepsipeptide
with improved activity for instance against human worm infections new
derivatives are required. We detail here for the first time the synthesis of phenylheteroaromatic
analogues of PF1022A prepared by efficient click-reactions.
Keywords: Anthelmintic, click-chemistry, cyclodep, heteroaromatic analogues, PF1022A, sipeptide.
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