In 2012,Journal of Biological Chemistry included an article by Kroth, Heiko; Ansaloni, Annalisa; Varisco, Yvan; Jan, Asad; Sreenivasachary, Nampally; Rezaei-Ghaleh, Nasrollah; Giriens, Valerie; Lohmann, Sophie; Lopez-Deber, Maria Pilar; Adolfsson, Oskar; Pihlgren, Maria; Paganetti, Paolo; Froestl, Wolfgang; Nagel-Steger, Luitgard; Willbold, Dieter; Schrader, Thomas; Zweckstetter, Markus; Pfeifer, Andrea; Lashuel, Hilal A.; Muhs, Andreas. Recommanded Product: 192701-73-8. The article was titled 《Discovery and Structure Activity Relationship of Small Molecule Inhibitors of Toxic β-Amyloid-42 Fibril Formation》. The information in the text is summarized as follows:
Increasing evidence implicates Aβ peptides self-assembly and fibril formation as crucial events in the pathogenesis of Alzheimer disease. Thus, inhibiting Aβ aggregation, among others, has emerged as a potential therapeutic intervention for this disorder. Herein, we employed 3-aminopyrazole as a key fragment in our design of non-dye compounds capable of interacting with Aβ42 via a donor-acceptor-donor hydrogen bond pattern complementary to that of the β-sheet conformation of Aβ42. The initial design of the compounds was based on connecting two 3-aminopyrazole moieties via a linker to identify suitable scaffold mols. Addnl. aryl substitutions on the two 3-aminopyrazole moieties were also explored to enhance π-π stacking/hydrophobic interactions with amino acids of Aβ42. The efficacy of these compounds on inhibiting Aβ fibril formation and toxicity in vitro was assessed using a combination of biophys. techniques and viability assays. Using structure activity relationship data from the in vitro assays, we identified compounds capable of preventing pathol. self-assembly of Aβ42 leading to decreased cell toxicity. In the experiment, the researchers used many compounds, for example, Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8Recommanded Product: 192701-73-8)
Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Recommanded Product: 192701-73-8
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics