Abstract

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.

Graphical Abstract