What question did this study set out to answer?

This work aims to design and synthesize new pyrimidinedione derivatives as safer protoporphyrinogen IX oxidase inhibitors.

April 25, 2026

Design and Synthesis of Novel Pyrimidinedione Derivatives Containing Dithioacetal Structures as Safer Protoporphyrinogen IX Oxidase Inhibitors

Key Points

This work aims to design and synthesize new pyrimidinedione derivatives as safer protoporphyrinogen IX oxidase inhibitors.
Integrated the antiviral disulfide acetal moiety into pyrimidinedione scaffold.
Conducted postemergence herbicidal activity assays on synthesized compounds.
Measured PPO inhibition potency using IC50 values against a reference drug.
Compound S1 exhibited over 80% weed control at 4.7 g a.i./ha.
S1 demonstrated an IC50 of 0.0151 μM, superior to saflufenacil with an IC50 of 0.0181 μM.
Compound S1 is safe for rice and wheat at a dose of 150 g a.i./ha.

Abstract

Protoporphyrinogen IX oxidase (PPO, EC 1.3.3.4) is a hot spot in the research of green herbicide targets and is often used to prepare novel and efficient herbicides. In this work, we integrated the antiviral disulfide acetal moiety into a pyrimidinedione scaffold, leading to the design and synthesis of a series of novel pyrimidinedione derivatives. The results of the postemergence herbicidal activity assay showed that the majority of the synthesized compounds exhibited significant herbicidal efficacy. Notably, compound S1 controls over 80% of various weeds at only 4.7 g a.i./ha. Further PPO activity experiments showed that compound S1 (IC50 = 0.0151 μM) demonstrated superior PPO inhibition over the reference drug saflufenacil (IC50 = 0.0181 μM). Additionally, at a dose of 150 g a.i./ha, compound S1 is safe for both rice and wheat. Therefore, S1 can be considered a lead for the development of efficient and safe PPO inhibitors.

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