Abstract：
The discovery of readily available and easily modifiable new models is a crucial and practical solution for agrochemical innovation. Antifungal function-oriented fusion of triazole with the prevalidated lead (R)-LE001 affords a novel framework with a broad and enhanced antifungal spectrum. Characterized by the easy accessibility and adjustability of [1,2,4]triazolo[4,3-a]pyridine, modular fine-tuning provided a set of unprecedented leads (e.g., Z23, Z25, Z26, etc.) with superior antifungal potentials than the positive control boscalid. Candidate Z23 exhibited a more promising antifungal activity against Sclerotinia sclerotiorum, Botrytis cinerea, and Phytophthora capsici with EC50 values of 0.7, 0.6, and 0.5 μM, respectively. This candidate could effectively control boscalid-resistant B. cinerea strains and also exhibit good vivo efficacy in controlling gray mold. Noteworthily, both the SDH-inhibition and the efficiency against Oomycete P. capsici are quite distinct from that of the positive control boscalid. A molecular docking simulation also differentiates Z23 from boscalid. These findings highlight the potential of [1,2,4]triazolo[4,3-a]pyridine amide as a novel antifungal model.
摘要：
发现容易获得和易于修改的新模型是农业化学创新的关键和实用的解决方案。以抗真菌功能为导向的三唑与预先验证的铅（R）-LE001融合提供了具有广泛且增强的抗真菌谱的新型框架。以[1,2,4]三唑并[4,3-a]吡啶的易接近性和可调性为特征，模块化微调提供了一组前所未有的线索(例如，Z23、Z25、Z26等。)具有比阳性对照物更好的抗真菌潜力。候选Z23对菌核病显示出更有希望的抗真菌活性，灰葡萄孢菌,和辣椒疫霉，EC50值为0.7、0.6和0.5μM，分别。该候选物可以有效地控制抗啶酰菌液的灰霉病菌菌株，并且在控制灰霉病方面也表现出良好的体内功效。值得注意的是,SDH抑制和抗卵菌P.capsici的效率都与阳性对照物非常不同。分子对接模拟也将Z23与啶酰菌胺区分开。这些发现强调了[1,2,4]三唑并[4,3-a]吡啶酰胺作为新型抗真菌模型的潜力。
