Aminoisothiazolamides, a new class of potent inhibitors of lysyl-tRNA synthetase.

ABSTRACT:

Background

Owing to the economic relevance of resistance evolution against herbicides, new chemical entities addressing unprecedented molecular targets are urgently needed to develop future sustainable weed control solutions. As part of our discovery research, the new class of aminoisothiazolamides was investigated.

Results

Aminoisothiazolamide 3-amino-4-chloro-N-(cyclohexylmethyl)isothiazole-5-carboxamide 1a and several of its derivatives displayed potent herbicidal and fungicidal in vivo activity in initial glasshouse tests. Lysyl-tRNA synthetase 1 (KRS1) was identified as the putative target for 1a and was validated as a key contributor to the biochemical mode-of-action of aminoisothiazolamides. Thermal stability shift analysis with KRS1 from Arabidopsis thaliana (AtKRS1)

SUBMITTER: Bernier D 

PROVIDER: S-EPMC12159408 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature