59052-85-6

Usage

Uses

Used in Pharmaceutical Industry:
2-PIPERAZIN-1-YLMETHYL-1H-BENZOIMIDAZOLE is used as a potential active pharmaceutical ingredient for the development of medications targeting various conditions. Its unique structure, featuring a piperazine and benzimidazole ring, suggests that it may interact with biological systems in ways that could be therapeutically beneficial. The specific applications and effects of 2-PIPERAZIN-1-YLMETHYL-1H-BENZOIMIDAZOLE in medicinal chemistry are yet to be fully understood and require additional research and development.

Upstream product

• 95-54-5 1,2-diamino-benzene 
• 110-85-0 piperazine 
• 4857-04-9 2-chloromethyl-1H-benzimidazole 

Downstream Products

• 1354972-24-9 1-(4-((1H-benzo[d]imidazol-2-yl)methyl)piperazin-1-yl)-2-(2,4-difluoro phenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol 

Relevant academic research and scientific papers

Design, synthesis, characterization and evaluation of 1,3,5-triazine-benzimidazole hybrids as multifunctional acetylcholinesterases inhibitors

A series of hybrids of benzimidazole and 1,3,5-triazine were designed and synthesized and evaluated as multi-target agents for the treatment of Alzheimer's disease. 24 compounds were designed, synthesized and identified by NMR, IR, HRMS and single-crystal X-ray diffraction studies. The compound 6c had the crystal system of orthorhombic and the space group of P212121. The cholinesterase inhibitory activity of synthesized compounds was measured using colorimetric Ellman's method. Most 1,3,5-triazine-benzimidazole hybrids showed potent acetylcholinesterase-inhibition activities and weak butyrylcholinesterase inhibitory activities. Compound 9f possessed the best acetylcholinesterase inhibitory activity with the IC50 of 0.044 μM, which is better than donepezil (0.052 μM). Molecular docking and molecular dynamics simulations demonstrated that there is a stable interaction between compound 9f and acetylcholinesterase. Simultaneously, experiments have also proved that compound 9f has good metal chelating properties. ADMET in silico prediction results suggest the compound can pass through the blood-brain barrier well and have good drug similarity. So, compound 9f could be a multi-target agent for the treatment of Alzheimer's disease.

One-pot multicomponent synthesis of novel 2-(piperazin-1-yl) quinoxaline and benzimidazole derivatives, using a novel sulfamic acid functionalized Fe3O4 MNPs as highly effective nanocatalyst

The immobilization of sulfonic acid on the surface of Fe3O4 magnetic nanoparticles (MNPs) as a novel acid nanocatalyst has been successfully reported. The morphological features, thermal stability, magnetic properties, and other physicochemical properties of the prepared superparamagnetic core–shell (Fe3O4@PFBA–Metformin@SO3H) were thoroughly characterized using Fourier transform infrared (FTIR), X-ray diffraction (XRD), energy-dispersive X-ray spectroscopy (EDS), field-emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), thermogravimetric analysis–differential thermal analysis (TGA-DTA), atomic force microscopy (AFM), dynamic light scattering (DLS), Brunauer–Emmett–Teller (BET), and vibrating sample magnetometer (VSM) techniques. It was applied as an efficient and reusable catalyst for the synthesis of 2-(piperazin-1-yl) quinoxaline and benzimidazole derivatives via a one-pot multiple-component cascade reaction under green conditions. The results displayed the excellent catalytic activity of Fe3O4@PFBA–metformin@SO3H as an organic–inorganic hybrid nanocatalyst in condensation and multicomponent Mannich-type reactions. The easy separation, simple workup, excellent stability, and reusability of the nanocatalyst and quantitative yields of products and short reaction time are some outstanding advantages of this protocol.

PYRAZOLOPYRIMIDIN-2-YL DERIVATIVES AS JAK INHIBITORS

New pyrazolopyridmiin-2-yl derivatives are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).