New Heteroaromatic Derivatives of the Anthelmintic Cyclooctadepsipeptide PF1022A by Click-Chemistry

Author(s): Sivatharushan Sivanathan, Julian Vollrodt, Jürgen Scherkenbeck.

Journal Name: Letters in Organic Chemistry

Volume 13 , Issue 6 , 2016

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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.

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Article Details

VOLUME: 13
ISSUE: 6
Year: 2016
Page: [441 - 445]
Pages: 5
DOI: 10.2174/1570178613666160502161309
Price: $58

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