Imidazole is a five-membered heterocyclic moiety that possesses three carbon, two nitrogen, four hydrogen atoms, and two double bonds. 1739-84-0, formula is C5H8N2, Name is 1,2-Dimethyl-1H-imidazole. It is also known as 1, 3-diazole. It contains two nitrogen atoms, in which one nitrogen bear a hydrogen atom, and the other is called pyrrole type nitrogen. Category: imidazoles-derivatives.
Barlaam, Bernard;Casella, Robert;Cidado, Justin;Cook, Calum;De Savi, Chris;Dishington, Allan;Donald, Craig S.;Drew, Lisa;Ferguson, Andrew D.;Ferguson, Douglas;Glossop, Steve;Grebe, Tyler;Gu, Chungang;Hande, Sudhir;Hawkins, Janet;Hird, Alexander W.;Holmes, Jane;Horstick, James;Jiang, Yun;Lamb, Michelle L.;McGuire, Thomas M.;Moore, Jane E.;O’Connell, Nichole;Pike, Andy;Pike, Kurt G.;Proia, Theresa;Roberts, Bryan;San Martin, Maryann;Sarkar, Ujjal;Shao, Wenlin;Stead, Darren;Sumner, Neil;Thakur, Kumar;Vasbinder, Melissa M.;Varnes, Jeffrey G.;Wang, Jianyan;Wang, Lei;Wu, Dedong;Wu, Liangwei;Yang, Bin;Yao, Tieguang research published 《 Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies》, the research content is summarized as follows. A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the optimization of a series of amidopyridines (from compound 2), focusing on properties suitable for achieving short target engagement after i.v. administration. By increasing potency and human metabolic clearance, we identified compound 24, a potent and selective CDK9 inhibitor with suitable predicted human pharmacokinetic properties to deliver transient inhibition of CDK9. Furthermore, the solubility of 24 was considered adequate to allow i.v. formulation at the anticipated ED. Short-term treatment with compound 24 led to a rapid dose- and time-dependent decrease of pSer2-RNAP2 and Mcl-1, resulting in cell apoptosis in multiple hematol. cancer cell lines. Intermittent dosing of compound 24 demonstrated efficacy in xenograft models derived from multiple hematol. tumors. Compound 24 is currently in clin. trials for the treatment of hematol. malignancies.
1739-84-0, 1,2-Dimethylimidazole is used in the synthesis of 1,2-dimethyl-3-n-butylimidazoliumchloride and 1,2-dimethyl-3-n-propylimidazolium chloride. It also can be used in the synthesis of 1-(2-methoxyethyl)-2,3-dimethylimidazolium chloride and hexafluorophosphate salts.
1,2-Dimethylimidazole is a heterocyclic compound that contains nitrogen and carbon. It can be produced by the reaction between glyoxal and fatty acid in the presence of a base. 1,2-Dimethylimidazole has been shown to have biological properties such as an antioxidant effect. It is also used as a chemical intermediate for production of other chemicals such as 2-methylimidazole and 3-methylimidazole. 1,2-Dimethylimidazole has been shown to react with metal carbonyls to produce methylimines, which are useful intermediates in organic synthesis. The reaction mechanism involves hydrogen bonding and steric interactions between the imidazole ring and the metal carbonyl reactant., Category: imidazoles-derivatives
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem