In 2019,Pesticide Biochemistry and Physiology included an article by Yan, Wei; Wang, Xing; Li, Ke; Li, Tian-Xi; Wang, Jia-Jie; Yao, Kai-Cheng; Cao, Ling-Ling; Zhao, Shuang-Shuang; Ye, Yong-Hao. Category: triazoles. The article was titled 《Design, synthesis, and antifungal activity of carboxamide derivatives possessing 1,2,3-triazole as potential succinate dehydrogenase inhibitors》. The information in the text is summarized as follows:
Succinate dehydrogenase (SDH) is demonstrably one of the most important mol. targets in development of new fungicide. In our continuous efforts to discover novel SDH inhibitors, forty-two carboxamide derivatives containing 1,2,3-triazole ring were designed and synthesized, which were precisely characterized by 1H NMR, ESI-MS, elemental anal. and X-ray single-crystal diffraction. The compounds were screened for antifungal activities against phytopathogenic fungi by mycelia growth inhibition assay in vitro. Compound A3-3 exhibited significant antifungal activity against Sclerotinia sclerotiorum, Botrytis cinerea, Rhizoctonia cerealis and Gaeumannomyces graminsis with EC50 values of 1.08, 8.75, 1.67 and 5.30μg/mL, resp., comparable to those of com. SDHI boscalid. In vivo testing demonstrated that A3-3 was effective for suppressing rape sclerotinia rot, cucumber gray mold and wheat powdery mildew caused by S. sclerotiorum, B. cinerea and Blumeria graminis at a dosage of 200μg/mL. Inhibition activities against SDH test proved the designed analogs were effective in the enzyme level. The mol. docking simulation revealed that A3-3 interacted with ARG43, TYR58 and TRP173 of the SDH through hydrogen bond and pi-pi interaction, which could explain the probable mechanism of action between the inhibitor and target protein.1H-1,2,3-Triazole(cas: 288-36-8Category: triazoles) was used in this study.
1H-1,2,3-Triazole(cas: 288-36-8) belongs to triazoles. Triazoles are an important group of nitrogen-containing five-membered heterocyclic scaffolds. Triazoles are core structures of several drugs and pharmaceutical agents. Triazole derivatives possess antimicrobial, antiparasitic, antidiabetic, analgesic, and anti-inflammatory properties Category: triazoles
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics