Controllable Soil Degradation Rate of 5‑Substituted Sulfonylurea Herbicides as Novel AHAS Inhibitors

Chlorsulfuron has been applied in
wheat fields as a recognized
herbicide worldwide, yet it was officially banned in China since 2014
for its soil persistence problem. On the basis of our previous research
that 5-dimethylamino distinctively accelerated degradation rate in
soils, a modified amino moiety (Ia-c) and monosubstituted
amino group (Id-e) were introduced onto the fifth position
of the benzene ring in sulfonylurea structures, as well as heterocyclic
amino substituents (If-g) to seek a suitable soil degradation
rate during such an in situ crop rotation system. Referring to the
biological data and ScAHAS inhibition and ScAHAS docking results, they turned out to be AHAS inhibitors
with high potent herbicidal activities. The various influence on soil
degradation rate along with crop safety indicated that different substituents
on the fifth position have exerted an apparent impact. Their united
study of structure–activity–safety–degradation
relationship has great potential to provide valuable information for
further development of eco-friendly agrochemicals.