59282-87-0Relevant academic research and scientific papers
A practical synthesis of 2,4(5)-diarylimidazoles from simple building blocks
Zuliani, Valentina,Cocconcelli, Giuseppe,Fantini, Marco,Ghiron, Chiara,Rivara, Mirko
, p. 4551 - 4553 (2007)
(Chemical Equation Presented) A simple and efficient approach to selectively obtain 2,4(5)-diarylimidazoles suppressing formation of 2-aroyl-4(5)-arylimidazoles is described. The yield of each of the two products strongly depends on the reaction condition
A facile and eco-friendly synthesis of diarylthiazoles and diarylimidazoles in water
Kumar, Dalip,Kumar, N. Maruthi,Patel, Gautam,Gupta, Sudeep,Varma, Rajender S.
experimental part, p. 1983 - 1986 (2011/04/25)
A simple, efficient and high yielding greener protocol for the synthesis of substituted thiazoles and imidazoles is described that utilizes the reaction of readily available α-tosyloxy ketones with variety of thioamides/amidines in water.
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
scheme or table, 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.
