水稲用除草剤「イプトリアゾピリド」の作用メカニズムを解明

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2025-06-11 日産化学株式会社

日産化学と産総研は、新規水稲用除草剤「イプトリアゾピリド」の作用機序を解明した。この化合物はアゾールカルボキサミド構造を持つ初のHPPD阻害剤で、標的酵素に不可逆結合し、ヒエなどの耐性雑草に高い除草効果を示す。一方、イネ体内では速やかに分解されるため高い安全性を持ち、直播栽培への適性も高い。水稲栽培における労力や水使用量、メタン排出の削減にも寄与する。論文は『Journal of Agricultural and Food Chemistry』に掲載され、2027年の上市を目指す。

<関連情報>

イプトリアゾピリドの除草作用機構とイネ選択性:4-ヒドロキシフェニルピルビン酸ジオキシゲナーゼの新規アゾールカルボキサミド系阻害剤 Mechanism of Herbicidal Action and Rice Selectivity of Iptriazopyrid: A Novel Azole Carboxamide-Based Inhibitor of 4-Hydroxyphenylpyruvate Dioxygenase

Takashi Nishio,Nanami Nishijima,Tomomi Kubota,Yuichi Furuhata,Yoshiki Nanao,Hadian Permana,Takamasa Furuhashi,and Yoshio Kato
Journal of Agricultural and Food Chemistry  Published: June 10, 2025
DOI:https://doi.org/10.1021/acs.jafc.4c11831

Abstract

水稲用除草剤「イプトリアゾピリド」の作用メカニズムを解明

4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitors are widely used as herbicides. However, the emergence of herbicide-resistant weeds necessitates the development of new herbicides with more diverse chemical structures. Therefore, we evaluated the herbicidal and HPPD inhibitory activities of iptriazopyrid, a novel azole carboxamide compound. Phytotoxic tests on Echinochloa crus-galli demonstrated that iptriazopyrid caused chlorosis at a concentration approximately 10 times lower than that required for the common commercial HPPD inhibitor mesotrione. Furthermore, iptriazopyrid showed strong selectivity for Oryza sativa over the weed in the greenhouse-scale experiment. X-ray crystallography and in vitro inhibitory assays revealed that iptriazopyrid was bound to the enzyme active pocket of HPPD and worked as a slow-binding inhibitor. These findings indicate that this inhibitor has potent herbicidal activity with a chemical structure different from those of existing HPPD inhibitors. Thus, it has potential applications as a novel scaffold in herbicide development.

1202農芸化学
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