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. COA of Formula: C3H3N3O2.
George, Dawn M.;Huntley, Raymond J.;Cusack, Kevin;Duignan, David B.;Hoemann, Michael;Loud, Jacqueline;Mario, Regina;Melim, Terry;Mullen, Kelly;Somal, Gagandeep;Wang, Lu;Edmunds, Jeremy J. research published 《 Prodrugs for colon-restricted delivery: design, synthesis, and in vivo evaluation of colony stimulating factor 1 receptor (CSF1R) inhibitors》, the research content is summarized as follows. The ability to restrict low mol. weight compounds to the gastrointestinal (GI) tract may enable an enhanced therapeutic index for mol. targets known to be associated with systemic toxicity. Using a triazolopyrazine CSF1R inhibitor scaffold, a broad range of prodrugs were synthesized and evaluated for enhanced delivery to the colon in mice. Subsequently, the preferred cyclodextrin prodrug moiety was appended to a number of CSF1R inhibitory active parent mols., enabling GI-restricted delivery. Evaluation of a cyclodextrin prodrug in a dextran sodium sulfate (DSS)-induced mouse colitis model resulted in enhanced GI tissue levels of active parent. At a dose where no significant depletion of systemic monocytes were detected, the degree of pharmacodynamic effect-measured as reduction in macrophages in the colon-was inferior to that observed with a systemically available pos. control. This suggests that a suitable therapeutic index cannot be achieved with CSF1R inhibition by using GI-restricted delivery in mice. However, these efforts provide a comprehensive frame-work in which to pursue addnl. gut-restricted delivery strategies for future GI targets.
COA of Formula: C3H3N3O2, 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