Ma, ZH; Jiang, L; Li, GX; Liang, DL; Li, LF; Liu, L; Jiang, C in [Ma, Zonghui; Li, Guoxin; Liang, Dailin; Jiang, Cheng] China Pharmaceut Univ, Jiang Su Key Lab Drug Design & Optimizat, Tongjiaxiang 24, Nanjing 210009, Peoples R China; [Ma, Zonghui; Li, Guoxin; Liang, Dailin; Li, Luanfeng; Jiang, Cheng] China Pharmaceut Univ, Dept Med Chem, Tongjiaxiang 24, Nanjing 210009, Peoples R China; [Jiang, Ling; Liu, Li] China Pharmaceut Univ, Key Lab Drug Metab & Pharmacokinet, Tongjiaxiang 24, Nanjing 210009, Peoples R China published Design, synthesis of 1,3-dimethylpyrimidine-2,4-diones as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity in 2020, Cited 21. Recommanded Product: 62-23-7. The Name is 4-Nitrobenzoic acid. Through research, I have a further understanding and discovery of 62-23-7.
LDH1A1, one of 19 NAD(P)(+)-dependent aldehyde dehydrogenases, participates in multiple metabolic pathways and has been indicated to play an important role in obesity and diabetes. In this study, a series of 1,3-di-methylpyrimidine-2,4-diones were designed, synthesized and evaluated as novel selective aldehyde dehy-drogenase 1A1 inhibitors. Among them, compounds 46, 50, 53, 56 and 57 exhibited excellent inhibitory activity against ALDH1A1 with IC50 values in the low nanomolar range and high selectivity over ALDH1A2, ALDH1A3, ALDH2 and ALDH3A1. Furthermore, in vitro study demonstrated that compound 57 effectively improved glucose consumption in HepG2 cells compared to compound 1 (CM026).
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Reference:
Phthalazine – Wikipedia,
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