Discovery and Optimization of Spirocyclic Lactams that Inhibit Acyl-ACP Thioesterase.

The present work covers a series of novel herbicidal lead structures that contain a spirocyclic lactam as a structural key feature carrying ortho-substituted benzyl or heteroarylmethylene side chains. These new compounds show good acyl-ACP thioesterase inhibition in line with strong herbicidal activity. Greenhouse trials showed that the spirolactams outlined herein display promising control of grass-weed species in pre-emergence application combined with dose response windows that enable partial selectivity in wheat and corn. Remarkably, some of the novel acyl-ACP thioesterase-inhibitors showed efficacy against resistant grass weeds such as Alopecurus myosuroides and Lolium species on competitive levels compared with commercial standards. This article is protected by copyright. All rights reserved.