38385-95-4

Usage

Uses

Used in Pharmaceutical Industry:
2-PIPERIDIN-4-YL-1H-BENZOIMIDAZOLE is used as a potential anti-cancer agent for its ability to target and inhibit the growth of cancer cells. Its unique structure allows it to interact with specific biological targets, making it a promising candidate for the development of new cancer therapies.
2-PIPERIDIN-4-YL-1H-BENZOIMIDAZOLE is also used as a potential treatment for psychiatric disorders due to its potential to modulate neurotransmitter systems and alleviate symptoms associated with these conditions.
Furthermore, 2-PIPERIDIN-4-YL-1H-BENZOIMIDAZOLE is used as a potential treatment for infectious diseases, leveraging its ability to target and inhibit the replication of pathogens, thereby contributing to the development of new antimicrobial agents.

InChI:InChI=1/C12H15N3/c1-2-4-11-10(3-1)14-12(15-11)9-5-7-13-8-6-9/h1-4,9,13H,5-8H2,(H,14,15)

Upstream product

• 498-94-2 isonipecotic acid 
• 95-54-5 1,2-diamino-benzene 
• 953071-73-3 tert-butyl 4-(1H-benzo[d]imidazol-2-yl)piperidine-1-carboxylate 

Downstream Products

• 845539-62-0 2-[1-(4-Chloro-benzyl)-piperidin-4-yl]-1H-benzoimidazole 
• 154541-63-6 2-[1-(4-tert-Butyl-benzyl)-piperidin-4-yl]-1H-benzoimidazole 
• 887217-03-0 2-[1-(2-Chloro-benzyl)-piperidin-4-yl]-1H-benzoimidazole 
• 400797-32-2 1-[1-{3-[4-(1H-Benzoimidazol-2-yl)-piperidin-1-yl]-2-hydroxy-propyl}-3-(4-trifluoromethyl-phenyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone 
• 1159096-73-7 (4-(1H-benzo[d]imidazol-2-yl)piperidin-1-yl)(4'-(trifluoromethoxy)-[1,1'-biphenyl]-4-yl)methanone 
• 1159096-67-9 [4-(1H-benzimidazol-2-yl)piperidin-1-yl][4-(pyridin-2-yl)phenyl]methanone 
• 1159096-70-4 C₂₄H₂₈N₄O 
• 605627-96-1 [4-(1H-benzimidazol-2-yl)piperidin-1-yl](4-bromophenyl)methanone 
• 1159096-69-1 C₂₅H₂₉N₃O 
• 1159096-75-9 C₂₅H₂₉N₃O 
• 1159096-72-6 [4-(1H-benzimidazol-2-yl)piperidin-1-yl](4'-methoxybiphenyl-4-yl)methanone 
• 1159096-79-3 C₂₅H₂₅N₅O₂ 
• 1159096-81-7 2-[1-(biphenyl-4-ylsulfonyl)piperidin-4-yl]-1H-benzimidazole 
• 1159096-77-1 [4-(1H-benzimidazol-2-yl)piperidin-1-yl](2-phenylpyrimidin-5-yl)methanone 

Relevant academic research and scientific papers

Substituted benzimidazoles as modulators of Ras signaling

Benzimidazole compounds that increase the rate of SOS-mediated nucleotide exchange on Ras by binding to a functionally relevant, chemically tractable pocket on the SOS protein, as part of the Ras:SOS:Ras complex.

IMPROVED PROCESSES FOR PREPARATION OF BILASTINE USING NOVEL INTERMEDIATES

Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of Bilastine or a pharmaceutically acceptable salt thereof using novel intermediates, in high yield and purity.

Discovery of Novel 2-(piperidin-4-yl)-1H-benzo[d]imidazole Derivatives as Potential Anti-Inflammatory Agents

A novel 2-(piperidin-4-yl)-1H-benzo[d]imidazole derivative 5 with good anti-inflammatory activity was identified from our in-house library. Based on hit compound 5, two series of 2-(piperidin-4-yl)-1H-benzo[d]imidazole derivative 6a-g and 7a-h were designed and synthesized as novel anti-inflammatory agents. Most of synthesized compounds exhibited good inhibitory activity on NO and TNF-α production in LPS-stimulated RAW 264.7 macrophages, in which the compound 6e showed most potent inhibitory activity on NO (IC50 = 0.86 μm) and TNF-α (IC50 = 1.87 μm) production. Further evaluation revealed that compound 6e displayed more potent in vivo anti-inflammatory activity than ibuprofen did on xylene-induced ear oedema in mice. Additionally, Western blot analysis revealed that compound 6e could restore phosphorylation level of IκBα and protein expression of p65 NF-κB in LPS-stimulated RAW 264.7 macrophages.

Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site

K-Ras is one of the most frequently mutated signal transducing human oncogenes. Ras signaling activity requires correct cellular localization of the GTPase. The spatial organization of K-Ras is controlled by the prenyl binding protein PDEδ, which enhances Ras diffusion in the cytosol. Inhibition of the Ras-PDEδ interaction by small molecules impairs Ras localization and signaling. Here we describe in detail the identification and structure guided development of Ras-PDEδ inhibitors targeting the farnesyl binding pocket of PDEδ with nanomolar affinity. We report kinetic data that characterize the binding of the most potent small molecule ligands to PDEδ and prove their binding to endogenous PDEδ in cell lysates. The PDEδ inhibitors provide promising starting points for the establishment of new drug discovery programs aimed at cancers harboring oncogenic K-Ras.

DIPHENYLBUTYPIPERIDINE AUTOPHAGY INDUCERS

Autophagy inducing compounds, methods of their preparation and use, and kits containg said compounds are disclosed herein.

Modifications to five-substituted 3,3-diethyl-4,5-dihydro-2(3H)- Furanones en route to novel muscarinic receptor ligands

Lead lactone-based ligands with modest affinity for muscarinic receptors were modified based on structure- activity relationship data in the literature to provide a new series of 5-substituted 4,5-dihydro-2(3H)-furanones. The modifications included the addition of various nitrogencontaining heterocycles attached to substituted and unsubstituted aromatic rings. The target compounds were synthesized in modest yields and evaluated in preliminary muscarinic binding assays. A lactone-based ligand containing a diphenylmethylpiperazine moiety was identified as a nonselective muscarinic ligand with IC50 of 340 nM. The design of future ligands will be based, in part, on structure-activity data reported herein. Springer Science+Business Media, LLC 2011.

BRIDGED TETRAHYDRONAPHTHALENE DERIVATIVES

The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, A, B, W and n are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.

SEROTONIN 5-HT2B RECEPTOR INHIBITORS

Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds

A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties

We have been exploring the potential of 5-HT2B antagonists as a therapy for chronic heart failure. To assess the potential of this therapeutic approach, we sought compounds possessing the following attributes: (a) potent and selective antagonis

QUINOLONES USEFUL AS INDUCIBLE NITRIC OXIDE SYNTHASE INHIBITORS

The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.