Product Details of 62-23-7. Feng, JT; He, HF; Zhou, Y; Guo, XL; Liu, HL; Cai, M; Wang, F; Feng, LL; He, HW in [Feng, Jiangtao; He, Haifeng; Zhou, Yuan; Guo, Xiaoliang; Liu, Honglin; Cai, Meng; Wang, Fang; Feng, Lingling; He, Hongwu] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan 430079, Hubei, Peoples R China; [He, Haifeng] Jiangxi Sci & Technol Normal Univ, Sch Chem & Chem Engn, Nanchang 330013, Jiangxi, Peoples R China published Design, synthesis and biological evaluation of novel inhibitors against cyanobacterial pyruvate dehydrogenase multienzyme complex E1 in 2019.0, Cited 29.0. The Name is 4-Nitrobenzoic acid. Through research, I have a further understanding and discovery of 62-23-7.
Cyanobacterial pyruvate dehydrogenase multienzyme complex E1 (PDHc E1) is a potential target enzyme for finding inhibitors to control harmful cyanobacterial blooms. In this study, a series of novel triazole thiamin diphosphate (ThDP) analogs were designed and synthesized by modifying the substituent group of triazole ring and optimizing triazole-benzene linker as potential cyanobacterial PDHc E1 (Cy-PDHc E1) inhibitors. Their inhibitory activities against Cy-PDHc E1 in vitro and algicide activities in vivo were further examined. Most of these compounds exhibited prominent inhibitory activities against Cy-PDHc E1 (IC50 1.48-4.48 mu M) and good algicide activities against Synechocystis PCC6803 (EC50 0.84-2.44 mu M) and Microcystis aeruginosa FACHB905 (EC50 0.74-1.77 mu M). Especially, compound 8d showed not only the highest inhibitory activity against Cy-PDHc E1 (IC50 1.48 mu M), but also the most powerful inhibitory selectivity between Cy-PDHc E1 (inhibitory rate 98.90%) and porcine PDHc E1 (inhibitory rate only 9.54%). Furthermore, the potential interaction between compound 8d and Cy-PDHc E1 was analyzed by a molecular docking method and site-directed mutagenesis and enzymatic analysis and fluorescence spectral analysis. These results indicated that compound 8d could be used as a hit compound for further optimization and might have potential to be developed as a new algicide.
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