Tau-Centric Multitarget Approach for Alzheimer’s Disease: Development of First-in-Class Dual Glycogen Synthase Kinase 3β and Tau-Aggregation Inhibitors was written by Gandini, Annachiara;Bartolini, Manuela;Tedesco, Daniele;Martinez-Gonzalez, Loreto;Roca, Carlos;Campillo, Nuria E.;Zaldivar-Diez, Josefa;Perez, Concepcion;Zuccheri, Giampaolo;Miti, Andrea;Feoli, Alessandra;Castellano, Sabrina;Petralla, Sabrina;Monti, Barbara;Rossi, Martina;Moda, Fabio;Legname, Giuseppe;Martinez, Ana;Bolognesi, Maria Laura. And the article was included in Journal of Medicinal Chemistry in 2018.HPLC of Formula: 3012-80-4 This article mentions the following:
Several findings propose the altered tau protein network as an important target for Alzheimer’s disease (AD). Particularly, two points of pharmacol. intervention can be envisaged: inhibition of phosphorylating tau kinase GSK-3β and tau aggregation process. On the basis of this consideration and on the authors’ interest in multitarget paradigms in AD, the authors report on the discovery of 2,4-thiazolidinedione derivatives endowed with such a profile. 28 and 30 displayed micromolar IC50 values toward GSK-3β, together with the capacity of inhibiting AcPHF6 aggregation of 60% and 80% at 10 μM, resp. In addition, they showed PAMPA-BBB permeability, together with a suitable cellular safety profile. 30 also displayed inhibition of both K18 and full-length tau aggregations. Finally, both compounds were able to improve cell viability in an okadaic acid-induced neurodegeneration cell model. To the best of the authors’ knowledge, 28 and 30 are the first balanced, nontoxic, dual-acting compounds hitting tau cascade at two different hubs. In the experiment, the researchers used many compounds, for example, 1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde (cas: 3012-80-4HPLC of Formula: 3012-80-4).
1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde (cas: 3012-80-4) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with a Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.HPLC of Formula: 3012-80-4
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem