Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Reference of 2075-46-9.
Kapadia, Khushboo;Trojniak, Ashley E.;Guzman Rodriguez, Kenneth B.;Klus, Nicholas J.;Huntley, Coral;McDonald, Peter;Roy, Anuradha;Frankowski, Kevin J.;Aube, Jeffrey;Muma, Nancy A. research published 《 Small-Molecule Disruptors of Mutant Huntingtin-Calmodulin Protein-Protein Interaction Attenuate Deleterious Effects of Mutant Huntingtin》, the research content is summarized as follows. Huntington′s disease is a progressive and lethal neurodegenerative disease caused by an increased CAG repeat mutation in exon 1 of the huntingtin gene (mutant huntingtin). Current drug treatments provide only limited symptomatic relief without impacting disease progression. Previous studies in our lab and others identified the abnormal binding of mutant huntingtin protein with calmodulin, a key regulator of calcium signaling. Disrupting the abnormal binding of mutant huntingtin to calmodulin reduces perturbations caused by mutant huntingtin in cell and mouse models of Huntington′s disease and importantly normalizes receptor-stimulated calcium release. Using a series of high-throughput in vitro and cell-based screening assays, we identified numerous small-mol. hits that disrupt the binding of mutant huntingtin to calmodulin and demonstrate protective effects. Iterative optimization of one hit resulted in nontoxic, selective compounds that are protective against mutant huntingtin cytotoxicity and normalized receptor-stimulated intracellular calcium release in PC12 cell models of Huntington′s disease. Importantly, the compounds do not work by reducing the levels of mutant huntingtin, allowing this strategy to complement future mol. approaches to reduce mutant huntingtin expression. Our novel scaffold will serve as a prototype for further drug development in Huntington′s disease. These studies indicate that the development of small-mol. compounds that disrupt the binding of mutant huntingtin to calmodulin is a promising approach for the advancement of therapeutics to treat Huntington′s disease.
Reference of 2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.
4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics