Background:
Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) is a key enzyme in the biosynthesis
of chlorophyll and heme, also the target of different types of herbicides. Thiazole compounds
shown excellent biological activity, can be designed by using active groups docking for new
PPO inhibitors.
Objective:
The objective of this study was to synthsize a series of aryl thiazole compounds as PPO
inhibitors.
Methods:
In this study, a series of aryl thiazole compounds derivatives 11a-l were obtained from 2-
chloro-5-nitrobenzoic acid as the starting material via esterification, Iron powder reduction, diazotization,
Hantzsch reaction and final acylation. All synthesized compounds have been tested for their
herbicidal activities as a PPO inhibitors.
Results:
The Petri dish test indicated that all compounds exhibited good herbicidal activities at 200
mg/L using culture dish. And the post-emergence tests showed that at 150g.ai/ha on weed stem leaf
spray treatment, some of the title compounds exhibited 80% inhibition rate against the dicotyledonou
weeds Amaranthus retroflexus and Eclipta prostrate.
Conclusion:
Good activity was noted for some compounds that compounds 11a, 11b, 11c, 11g, 11h
had 80% inhibition on stems and leaves of Amaranthus retroflexus at 150g.ai/ha.