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DOI: 10.1055/s-0043-1775502
Synthesis and Biological Profile of Substituted Azetidinyl Carboxamides, A Novel Class of Herbicidal Acyl-ACP Thioesterase Inhibitors
Authors
L.R.C., C.M.P., L.P., and S.L. would like to thank the Herbicide Innovation Partnership (HIP) between the Grains Research and Development Corporation (GRDC) and Bayer AG for Postdoctoral Research Fellowships.
Dedicated to Klemens Minn on the occasion of his 70th birthday
Abstract
Utilizing scaffold hopping and bioisosteric replacement strategies, we explored new azetidinyl carboxamide inhibitors of the plant-specific enzyme acyl-ACP thioesterase (FAT). Amongst the investigated compounds we identified new structural motifs that showed promising target affinity coupled with good in vivo efficacy against commercially important weed species. We further studied the structure-activity relationship (SAR) of the novel azetidinyl pyrazole carboxamide scaffold which showed promise as a new type of FAT inhibiting herbicides. Accordingly, a focused synthetic approach towards azetidinyl carboxamides was explored.
Key words
herbicide - acyl-ACP thioesterase - azetidine - pyrazole carboxamide - structure-activity relationship - bioisosteresSupporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0043-1775502.
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Publication History
Received: 08 September 2025
Accepted after revision: 13 October 2025
Article published online:
10 November 2025
© 2025. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting copying and reproduction so long as the original work is given appropriate credit. Contents may not be used for commercial purposes or adapted, remixed, transformed or built upon. (https://creativecommons.org/licenses/by/4.0/)
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