111114-70-6Relevant academic research and scientific papers
Nickel-Catalyzed Construction of 2,4-Disubstituted Imidazoles via C–C Coupling and C?N Condensation Cascade Reactions
Fang, Shengyang,Yu, Haihua,Yang, Xicheng,Li, Jianqi,Shao, Liming
supporting information, p. 3312 - 3317 (2019/06/13)
A convenient Ni(II)-catalyzed C?C and C?N cascade coupling reaction was developed to directly access various 2,4-disubstituted imidazoles. The reaction scope covers a variety of aryl and aliphatic substitutions, which demonstrate moderate-to-excellent yie
Synthesis of Imidazoles and Pyrimidines Using Palladium-Catalyzed Decarboxylative Intramolecular Condensation of 1,2,4-Oxadiazol-5(4 H)-ones
Shimbayashi, Takuya,Okamoto, Kazuhiro,Ohe, Kouichi
, p. 1916 - 1920 (2014/08/18)
We found that 1,2,4-oxadiazol-5(4H)-ones acted as iminonitrene equivalents in the presence of a palladium catalyst and a stoichiometric amount of phosphine and that aza-Wittig-type condensation with the internal carbonyl moiety occurred to afford the corresponding imidazoles and pyrimidines. Georg Thieme Verlag Stuttgart. New York.
Anticonvulsant activity of 2,4(1H)-diarylimidazoles in mice and rats acute seizure models
Zuliani, Valentina,Fantini, Marco,Nigam, Aradhya,Stables, James P.,Patel, Manoj K.,Rivara, Mirko
experimental part, p. 7957 - 7965 (2011/01/13)
2,4(1H)-Diarylimidazoles have been previously shown to inhibit hNa V1.2 sodium (Na) channel currents. Since many of the clinically used anticonvulsants are known to inhibit Na channels as an important mechanism of their action, these compounds were tested in two acute rodent seizure models for anticonvulsant activity (MES and scMet) and for sedative and ataxic side effects. Compounds exhibiting antiepileptic activity were further tested to establish a dose response curve (ED50). The experimental data identified four compounds with anticonvulsant activity in the MES acute seizure rodent model (compound 10, ED50 = 61.7 mg/kg; compound 13, ED 50 = 46.8 mg/kg, compound 17, ED50 = 129.5 mg/kg and compound 20, ED50 = 136.7 mg/kg). Protective indexes (PI = TD 50/ED50) ranged from 2.1 (compound 10) to greater than 3.6 (compounds 13, 17 and 20). All four compounds were shown to inhibit hNa V1.2 in a dose dependant manner. Even if a correlation between sodium channel inhibition and anticonvulsant activity was unclear, these studies identify four Na channel antagonists with anticonvulsant activity, providing evidence that these derivatives could be potential drug candidates for development as safe, new and effective antiepileptic drugs (AEDs).
2,4(5)-Diarylimidazoles: Synthesis and biological evaluation of a new class of sodium channel blockers against hNav1.2
Rivara, Mirko,Baheti, Aparna R.,Fantini, Marco,Cocconcelli, Giuseppe,Ghiron, Chiara,Kalmar, Christopher L.,Singh, Natasha,Merrick, Ellen C.,Patel, Manoj K.,Zuliani, Valentina
experimental part, p. 5460 - 5462 (2009/05/26)
A small family of novel 2,4(5)-diarylimidazoles were prepared through a simple and efficient synthesis and evaluated as potential inhibitors of hNav1.2 sodium channel currents. One member of this series (4) exhibited profound inhibition of Nav1.2 currents, emerging as a promising lead compound for further structure-activity relationship studies for the development of novel sodium channel blockers.
