Wu, Zhibing; Park, Hyung-Yeon; Xie, Dewen; Yang, Jingxin; Hou, Shuaitao; Shahzad, Nasir; Kim, Chan Kyung; Yang, Song published an article on February 3 ,2021. The article was titled 《Synthesis, Biological Evaluation, and 3D-QSAR Studies of N-(Substituted pyridine-4-yl)-1-(substituted phenyl)-5-trifluoromethyl-1H-pyrazole-4-carboxamide Derivatives as Potential Succinate Dehydrogenase Inhibitors》, and you may find the article in Journal of Agricultural and Food Chemistry.Recommanded Product: 4-Amino-2-picoline The information in the text is summarized as follows:
To develop more potential succinate dehydrogenase (SDH) inhibitors, we designed and synthesized a novel series of N-(substituted pyridine-4-yl)-1-(substituted phenyl)-5-trifluoromethyl-1H-pyrazole-4-carboxamide derivatives, I [R1 = H, CH3, F, Cl; R2 = 2-pyridinyl, 4-pyridinyl, 2-CH3-4-pyridinyl, etc.]. The bioassay results demonstrated that some title compounds exhibited excellent antifungal activity against four tested phytopathogenic fungi (Gibberella zea, Fusarium oxysporum, Cytospora mandshurica, and Phytophthora infestans). The EC50 values were 1.8μg/mL for I [R1 = Cl; R2 = 4-pyridinyl] against G. zeae, 1.5 and 3.6μg/mL for I [R1 = Cl; R2 = 2-CH3-4-pyridinyl] against F. oxysporum and C. mandshurica, resp., and 6.8μg/mL for I [R1 = F; R2 = 2-CH3-4-pyridinyl] against P. infestans. The SDH enzymic activity testing revealed that the IC50 values of I [R1 = H; R2 = 4-pyridinyl], I [R1 = CH3; R2 = 4-pyridinyl], I [R1 = F; R2 = 2-CH3-4-pyridinyl], and penthiopyrad were 12.5, 135.3, 6.9, and 223.9μg/mL, resp. The mol. docking results of this series of title compounds with SDH model demonstrated that the compounds could completely locate inside of the pocket, the body fragment formed H bonds, and the Ph ring showed a π-π interaction with Arg59, suggesting that these novel 5-trifluoromethyl-pyrazole-4-carboxamide derivatives might target SDH. These results provided a benchmark for understanding the antifungal activity against the phytopathogenic fungus P. infestans and prompt us to discover more potent SDH inhibitors.4-Amino-2-picoline(cas: 18437-58-6Recommanded Product: 4-Amino-2-picoline) was used in this study.
4-Amino-2-picoline(cas: 18437-58-6) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Recommanded Product: 4-Amino-2-picoline