59282-86-9

Upstream product

• 500-22-1 3-pyridinecarboxaldehyde 
• 1074-12-0 phenylglyoxal hydrate 
• 7356-60-7 pyridine-3-carboxamidine hydrochloride 
• 70-11-1 α-bromoacetophenone 
• 4636-16-2 iodoacetophenone 
• 100-42-5 styrene 

Downstream Products

• 1057141-99-7 3-(1-methyl-4-phenyl-1H-imidazol-2-yl)-pyridine 

Relevant academic research and scientific papers

Direct preparation of thiazoles, imidazoles, imidazopyridines and thiazolidines from alkenes

A range of heterocycles, namely thiazoles, imidazoles, imidazopyridines, thiazolidines and dimethoxyindoles, have been synthesised directly from alkenes via a two-step ketoidoination/cyclisation protocol. The alkene starting materials are themselves readily accessible using many different and well-established approaches, and allow access to a variety of heterocycles with excellent yields and regioselectivity.

Direct preparation of heteroaromatic compounds from alkenes

A series of aromatic heterocycles, thiazoles, imidazoles, and dimethoxyindoles, can be synthesised directly from alkenes via a ketoiodination-cyclisation protocol. The alkene starting materials are themselves easily accessible by many different and well-established approaches, and allow access to various aromatic heterocycles with excellent yields and regioselectivity. Georg Thieme Verlag Stuttgart - New York.

Anticonvulsant activity of 2,4(1H)-diarylimidazoles in mice and rats acute seizure models

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

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.

A practical synthesis of 2,4(5)-diarylimidazoles from simple building blocks

(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

Neurokinin-3 receptor modulators: diaryl imidazole derivatives

The invention relates to compounds of general Formula I: wherein the variables are as defined herein. Also provided are pharmaceutical compositions comprising such compounds, and methods for treating patients suffering from a disorder responsive to neurok