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. Category: pyrazoles-derivatives.
Zak, Mark;Hanan, Emily J.;Lupardus, Patrick;Brown, David G.;Robinson, Colin;Siu, Michael;Lyssikatos, Joseph P.;Romero, F. Anthony;Zhao, Guiling;Kellar, Terry;Mendonca, Rohan;Ray, Nicholas C.;Goodacre, Simon C.;Crackett, Peter H.;McLean, Neville;Hurley, Christopher A.;Yuen, Po-wai;Cheng, Yun-Xing;Liu, Xiongcai;Liimatta, Marya;Kohli, Pawan Bir;Nonomiya, Jim;Salmon, Gary;Buckley, Gerry;Lloyd, Julia;Gibbons, Paul;Ghilardi, Nico;Kenny, Jane R.;Johnson, Adam research published 《 Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling》, the research content is summarized as follows. Disruption of interleukin-13 (IL-13) signaling with large mol. antibody therapies has shown promise in diseases of allergic inflammation. Given that IL-13 recruits several members of the Janus Kinase family (JAK1, JAK2, and TYK2) to its receptor complex, JAK inhibition may offer an alternate small mol. approach to disrupting IL-13 signaling. Herein we demonstrate that JAK1 is likely the isoform most important to IL-13 signaling. Structure-based design was then used to improve the JAK1 potency of a series of previously reported JAK2 inhibitors. The ability to impede IL-13 signaling was thereby significantly improved, with the best compounds exhibiting single digit nM IC50‘s in cell-based assays dependent upon IL-13 signaling. Appropriate substitution was further found to influence inhibition of a key off-target, LRRK2. Finally, the most potent compounds were found to be metabolically labile, which makes them ideal scaffolds for further development as topical agents for IL-13 mediated diseases of the lungs and skin (for example asthma and atopic dermatitis, resp.).
Category: pyrazoles-derivatives, 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