Discovery of metyltetraprole: Identification of tetrazolinone pharmacophore to overcome QoI resistance.,Bioorganic & Medicinal Chemistry

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Discovery of metyltetraprole: Identification of tetrazolinone pharmacophore to overcome QoI resistance.
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2019-11-09 , DOI: 10.1016/j.bmc.2019.115211
Yuichi Matsuzaki ₁ , Yuya Yoshimoto ₁ , Sadayuki Arimori ₁ , So Kiguchi ₁ , Toshiyuki Harada ₁ , Fukumatsu Iwahashi ₁

Affiliation

Quinone outside inhibitors (QoIs) are one of the major agricultural fungicide groups used worldwide. However, the development of resistance by different pathogenic species associated with specific mutation at the target gene site is becoming a critical issue for the sustainable use of QoIs. The authors aimed to design a novel QoI molecule to overcome the aforementioned issue. A rational approach to avoid steric hindrance between the QoI molecule and the mutated target site was successfully employed. The resulting compound, metyltetraprole, is characterized by 3-substituted central ring with a tetrazolinone moiety, the key structure to retain potent activity against QoI-resistant mutants. Metyltetraprole is a promising new fungicide under commercial development, and its development in this study has paved the way to overcoming resistance to QoI fungicides.

中文翻译：

甲基四甲基丙烯酰胺的发现：鉴定四唑啉酮药效团以克服QoI耐药性。

醌外抑制剂（QoIs）是全世界使用的主要农业杀真菌剂之一。然而，与目标基因位点的特定突变相关的不同病原体对耐药性的发展正成为可持续利用QoI的关键问题。作者旨在设计一种新颖的QoI分子来克服上述问题。成功地采用了一种合理的方法来避免QoI分子和突变的靶位点之间的空间位阻。所得的化合物甲戊四醇的特征是带有四唑啉酮部分的3个取代的中心环，这是保持对QoI抗性突变体有效活性的关键结构。甲etyltetraprole是一种有前途的新型杀菌剂，正在商业化开发中，

更新日期：2019-11-11

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