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A Study in Scaffold Hopping: Discovery and Optimization of Thiazolopyridines as Potent Herbicides That Inhibit Acyl-ACP Thioesterase.
Abel, Steven A G; Alnafta, Neanne; Asmus, Elisabeth; Bollenbach-Wahl, Birgit; Braun, Ralf; Dittgen, Jan; Endler, Anne; Frackenpohl, Jens; Freigang, Jörg; Gatzweiler, Elmar; Heinemann, Ines; Helmke, Hendrik; Laber, Bernd; Lange, Gudrun; Machettira, Anu; McArthur, Gillian; Müller, Thomas; Odaybat, Magdalena; Reingruber, Anna M; Roth, Sina; Rosinger, Christopher H; Schmutzler, Dirk; Schulte, Wolfgang; Stoppel, Rhea; Tiebes, Jörg; Volpin, Giulio; Barber, David M.
Afiliación
  • Abel SAG; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Alnafta N; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Asmus E; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Bollenbach-Wahl B; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Braun R; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Dittgen J; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Endler A; Targenomix GmbH, Am Mühlenberg 11, 14476, Potsdam, Germany.
  • Frackenpohl J; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Freigang J; Research and Development, Hit Discovery, Bayer AG, Crop Science Division, Alfred-Nobel-Straße 50, 40789, Monheim am Rhein, Germany.
  • Gatzweiler E; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Heinemann I; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Helmke H; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Laber B; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Lange G; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Machettira A; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • McArthur G; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Müller T; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Odaybat M; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Reingruber AM; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Roth S; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Rosinger CH; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Schmutzler D; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Schulte W; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Stoppel R; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Tiebes J; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Volpin G; Research and Development, Small Molecules Technologies, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
  • Barber DM; Research and Development, Weed Control Research, Bayer AG, Crop Science Division, Industriepark Höchst, 65926, Frankfurt am Main, Germany.
J Agric Food Chem ; 71(47): 18212-18226, 2023 Nov 29.
Article en En | MEDLINE | ID: mdl-37677080
In the search for new chemical entities that can control resistant weeds by addressing novel modes of action (MoAs), we were interested in further exploring a compound class that contained a 1,8-naphthyridine core. By leveraging scaffold hopping methodologies, we were able to discover the new thiazolopyridine compound class that act as potent herbicidal molecules. Further biochemical investigations allowed us to identify that the thiazolopyridines inhibit acyl-acyl carrier protein (ACP) thioesterase (FAT), with this being further confirmed via an X-ray cocrystal structure. Greenhouse trials revealed that the thiazolopyridines display excellent control of grass weed species in pre-emergence application coupled with dose response windows that enable partial selectivity in certain crops.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Herbicidas Idioma: En Revista: J Agric Food Chem Año: 2023 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Herbicidas Idioma: En Revista: J Agric Food Chem Año: 2023 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Estados Unidos