Mambwe, Dickson; Kumar, Malkeet; Ferger, Richard; Taylor, Dale; Njoroge, Mathew; Coertzen, Dina; Reader, Janette; van der Watt, Mariette; Birkholtz, Lyn-Marie; Chibale, Kelly published their research in ACS Medicinal Chemistry Letters in 2021. The article was titled 《Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against Plasmodium falciparum In Vitro》.Quality Control of 2-(2-Hydroxyethyl)pyridine The article contains the following contents:
In the context of drug repositioning and expanding the existing structure-activity relationship around astemizole (AST), a new series of analogs were designed, synthesized, and evaluated for their antiplasmodium activity. Among 46 analogs tested, compounds 21, 30, and 33 displayed high activities against asexual blood stage parasites (PfNF54 IC50 = 0.025-0.043μM), whereas amide compound 46 addnl. showed activity against late-stage gametocytes (stage IV/V; PfLG IC50 = 0.6 ± 0.1μM) and 860-fold higher selectivity over hERG (46, SI = 43) compared to AST. Several analogs displaying high solubility (Sol > 100μM) and low cytotoxicity in the Chinese hamster ovary (SI > 148) cell line have also been identified. The results came from multiple reactions, including the reaction of 2-(2-Hydroxyethyl)pyridine(cas: 103-74-2Quality Control of 2-(2-Hydroxyethyl)pyridine)
2-(2-Hydroxyethyl)pyridine(cas: 103-74-2) belongs to pyridine. In industry and in the lab, pyridine is used as a reaction solvent, particularly when its basicity is useful, and as a starting material for synthesizing some herbicides, fungicides, and antiseptics.Quality Control of 2-(2-Hydroxyethyl)pyridine