Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Formula: C3H3N3O2.
Dilger, Andrew K.;Pabbisetty, Kumar B.;Corte, James R.;De Lucca, Indawati;Fang, Tianan;Yang, Wu;Pinto, Donald J. P.;Wang, Yufeng;Zhu, Yeheng;Mathur, Arvind;Li, Jianqing;Hou, Xiaoping;Smith, Daniel;Sun, Dawn;Zhang, Huiping;Krishnananthan, Subramaniam;Wu, Dauh-Rurng;Myers, Joseph E. Jr.;Sheriff, Steven;Rossi, Karen A.;Chacko, Silvi;Zheng, Joanna J.;Galella, Michael A.;Ziemba, Theresa;Dierks, Elizabeth A.;Bozarth, Jeffrey M.;Wu, Yiming;Crain, Earl;Wong, Pancras C.;Luettgen, Joseph M.;Wexler, Ruth R.;Ewing, William R. research published 《 Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy》, the research content is summarized as follows. Factor XIa (FXIa) is an enzyme in the coagulation cascade thought to amplify thrombin generation but has a limited role in hemostasis. From preclin. models and human genetics, an inhibitor of FXIa has the potential to be an antithrombotic agent with superior efficacy and safety. Reversible and irreversible inhibitors of FXIa have demonstrated excellent antithrombotic efficacy without increased bleeding time in animal models (). Herein, we report the discovery of a novel series of macrocyclic FXIa inhibitors containing a pyrazole P2′ moiety. Optimization of the series for (pharmacokinetic) PK properties, free fraction, and solubility resulted in the identification of milvexian (BMS-986177/JNJ-70033093, 17, FXIa Ki = 0.11 nM) as a clin. candidate for the prevention and treatment of thromboembolic disorders, suitable for oral administration.
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., Formula: C3H3N3O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics