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Chimia (Aarau). 2017 Dec 1;71(12):845-850. doi: 10.2533/chimia.2017.845.

Investigating the Structure-Activity Relationship of the Insecticidal Natural Product Rocaglamide.

Author information

1
Syngenta Crop Protection AG Research Chemistry WST-810.3.18 CH-4332 Stein;, Email: roger_g.hall@syngenta.com.
2
Formerly Ciba Central Research, later Novartis Central Research laboratories, Macclesfield, UK.
3
Syngenta Crop Protection AG Research Chemistry WST-810.3.18 CH-4332 Stein.
4
Formerly Novartis Crop Protection, Basel, Switzerland.

Abstract

The natural product Rocaglamide (1), isolated from the tree Aglaia elliptifolia, is a compelling but also challenging lead structure for crop protection. In laboratory assays, the natural product shows highly interesting insecticidal activity against chewing pests and beetles, but also phytotoxicity on some crop plants. Multi-step syntheses with control of stereochemistry were required to probe the structure-activity relationship (SAR), and seek simplified analogues. After a significant research effort, just two areas of the molecule were identified which allow modification whilst maintaining activity, as will be highlighted in this paper.

PMID:
29289246
DOI:
10.2533/chimia.2017.845
[Indexed for MEDLINE]

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