Two-step screening method to identify 伪-synuclein aggregation inhibitors for Parkinson’s disease was written by Hideshima, Makoto;Kimura, Yasuyoshi;Aguirre, Cesar;Kakuda, Keita;Takeuchi, Toshihide;Choong, Chi-Jing;Doi, Junko;Nabekura, Kei;Yamaguchi, Keiichi;Nakajima, Kichitaro;Baba, Kousuke;Nagano, Seiichi;Goto, Yuji;Nagai, Yoshitaka;Mochizuki, Hideki;Ikenaka, Kensuke. And the article was included in Scientific Reports in 2022.Reference of 117976-90-6 The following contents are mentioned in the article:
Parkinson’s disease is a neurodegenerative disease characterized by the formation of neuronal inclusions of 伪-synuclein in patient brains. As the disease progresses, toxic 伪-synuclein aggregates transmit throughout the nervous system. No effective disease-modifying therapy has been established, and preventing 伪-synuclein aggregation is thought to be one of the most promising approaches to ameliorate the disease. In this study, we performed a two-step screening using the thioflavin T assay and a cell-based assay to identify 伪-synuclein aggregation inhibitors. The first screening, thioflavin T assay, allowed the identification of 30 mols., among a total of 1262 FDA-approved small compounds, which showed inhibitory effects on 伪-synuclein fibrilization. In the second screening, a cell-based aggregation assay, seven out of these 30 candidates were found to prevent 伪-synuclein aggregation without causing substantial toxicity. Of the seven final candidates, tannic acid was the most promising compound The robustness of our screening method was validated by a primary neuronal cell model and a Caenorhabditis elegans model, which demonstrated the effect of tannic acid against 伪-synuclein aggregation. In conclusion, our two-step screening system is a powerful method for the identification of 伪-synuclein aggregation inhibitors, and tannic acid is a promising candidate as a disease-modifying drug for Parkinson’s disease. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Reference of 117976-90-6).
Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. Imidazole is incorporated into many important biological compounds. The most pervasive is the amino acid histidine, which has an imidazole side-chain. Histidine is present in many proteins and enzymes, e.g. by binding metal cofactors, as seen in hemoglobin.Reference of 117976-90-6
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem