15965-57-8

Usage

Uses

Used in Pharmaceutical Industry:
1H-Benzimidazole, 2-chloro-4-methyl-(9CI) is used as an intermediate compound for the synthesis of various pharmaceutical drugs. Its unique structure and reactivity allow for the development of new drug molecules with potential therapeutic applications.
Used in Agrochemical Industry:
1H-Benzimidazole, 2-chloro-4-methyl-(9CI) is used as a building block in the synthesis of agrochemicals, such as pesticides and herbicides. Its chemical properties contribute to the development of effective and environmentally friendly agrochemical products.
Used in Organic Synthesis:
1H-Benzimidazole, 2-chloro-4-methyl-(9CI) is used as a versatile starting material for the synthesis of a wide range of organic compounds. Its reactivity and functional groups enable the creation of complex molecules for various applications, including the development of new materials and the improvement of existing ones.

Upstream product

• 19190-68-2 4-methylbenzimidazolone 
• 2687-25-4 3-methyl-1,2-benzenediamine 
• 19190-68-2 4-methyl-1,3-dihydro-2H-benzoimidazol-2-one 
• 530-62-1 1,1'-carbonyldiimidazole 

Downstream Products

• 1453097-14-7 3-methyl-1-(4-methyl-1H-benzimidazol-2-yl)-4-(phenylmethyl)-1H-pyrazol-5-ol 

Relevant academic research and scientific papers

Nonpolar isosteres of damaged DNA bases: Effective mimicry of mutagenic properties of 8-oxopurines

A substantial fraction of mutations that arise in the cell comes from oxidative damage to DNA bases. Oxidation of purine bases at the 8-position, yielding 8-oxo-G and 8-oxo-A, results in conformational changes (from anti to syn) that cause miscoding durin

Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening

Here we report the discovery of a selective inhibitor of Aurora A, a key regulator of cell division and potential anticancer target. We used the atom category extended ligand overlap score (xLOS), a 3D ligand-based virtual screening method recently developed in our group, to select 437 shape and pharmacophore analogs of reference kinase inhibitors. Biochemical screening uncovered two inhibitor series with scaffolds unprecedented among kinase inhibitors. One of them was successfully optimized by structure-based design to a potent Aurora A inhibitor (IC50 = 2 nM) with very high kinome selectivity for Aurora kinases. This inhibitor locks Aurora A in an inactive conformation and disrupts binding to its activator protein TPX2, which impairs Aurora A localization at the mitotic spindle and induces cell division defects. This phenotype can be rescued by inhibitor-resistant Aurora A mutants. The inhibitor furthermore does not induce Aurora B specific effects in cells.

QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS

There are disclosed a series of quinuclidines having the Formula (I). which bind to the nicotinic α7 receptor and may be useful for the treatment of disorders of the central nervous system.

NOVEL BENZIMIDAZOLE DERIVATIVE AND USE THEREOF

The present invention aims to provide a compound capable of inhibiting PCA-1 that can be a target for a novel treatment method of various diseases, and pharmaceutical use of the compound. A compound represented by the formula (I): wherein each symbol is a

Design and synthesis of prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors as anti-prostate cancer drugs

A series of 1-aryl-3,4-substituted-1H-pyrazol-5-ol derivatives was synthesized and evaluated as prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors to obtain a novel anti-prostate cancer drug. After modifying 1-(1H-benzimidazol-2-yl)-3,4-dimethyl-1H-pyrazol-5-ol (1), a hit compound found during random screening using a recombinant PCA-1/ALKBH3, 1-(1H-5- methylbenzimidazol-2-yl)-4-benzyl-3-methyl-1H-pyrazol-5-ol (35, HUHS015), was obtained as a potent PCA-1/ALKBH3 inhibitor both in vitro and in vivo. The bioavailability (BA) of 35 was 7.2% in rats after oral administration. As expected, continuously administering 35 significantly suppressed the growth of DU145 cells, which are human hormone-independent prostate cancer cells, in a mouse xenograft model without untoward effects.

Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole derivatives

Design, syntheses, and structure-activity relationships of a novel class of 2-{3-oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole NPY Y5 receptor antagonists are described. The benzimidazole structures were newly designed based on the urea linkage of our prototype Y5 receptor antagonists (2 and 3). By optimizing substituents on the benzimidazole core part of the lead compound 5a, we were able to develop a potent, orally available, and brain-penetrable Y5 selective antagonist (5k). Crown Copyright

Benzimidazole derivatives, preparation and therapeutic use thereof

The invention relates to benzimidazole derivatives of general formula (I) in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom R3 represents in particular a hydrogen atom or a (C1-C4)alkyl group, R4 represents in p

Benzimidazole derivatives, preparation and therapeutic use thereof

The invention relates to benzimidazole derivatives of general formula in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compo

Heterocyclic amines having central nervous system activity

Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: STR1 and pharmaceutically acceptable salts thereof wherein R1, R2, and R3 are independently hydrogen, C1-6 alkyl, alkenyl, or alkynyl, C3-10 cycloalkyl, or R1 and R2 are joined to form a C3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C1-6 alkyl halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO2, N, CH, CH2, CHCH3, C=O, C=S, C-SCH3, C=NH, C-NH2, C-NHCH3, C--NHCOOCH3, or C--NHCN. B is CH2, CH, C=O, N, NH or N--CH3 ; n is 0 or 1; and D is CH, CH2, C=O, O, N, NH or N--CH3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.