Category: 3584-66-5

Zhang, Lei; Chen, Xiaojie; Liu, Jun; Zhu, Qingzhang; Leng, Ying; Luo, Xiaomin; Jiang, Hualiang; Liu, Hong published their research in European Journal of Medicinal Chemistry on December 31 ,2012. The article was titled 《Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase》.Synthetic Route of C8H4Cl4N2 The article contains the following contents:

Dual-target-directed agents simultaneously inhibiting glycogen phosphorylase (GP) and activating glucokinase (GK) could decelerate the inflow of glucose from glycogenolysis and accelerate the outflow of glucose in the liver, and therefore allow for better control over hyperglycemia in a synergetic manner. A series of hybrid compounds were designed by structure-assisted and ligand-based strategies. In vitro bioassays found two novel compounds I and II worthy of further optimization on balance of dual action to GP and GK. In addition, for single-target activity, two compounds exhibited more potent GP inhibitory activity and four compounds showed better GK activation than their corresponding references In the experiment, the researchers used many compounds, for example, 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5Synthetic Route of C8H4Cl4N2)

5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5) belongs to imidazoles.Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine. Synthetic Route of C8H4Cl4N2 In addition, imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Venable, Jennifer D.; Cai, Hui; Chai, Wenying; Dvorak, Curt A.; Grice, Cheryl A.; Jablonowski, Jill A.; Shah, Chandra R.; Kwok, Annette K.; Ly, Kiev S.; Pio, Barbara; Wei, Jianmei; Desai, Pragnya J.; Jiang, Wen; Nguyen, Steven; Ling, Ping; Wilson, Sandy J.; Dunford, Paul J.; Thurmond, Robin L.; Lovenberg, Timothy W.; Karlsson, Lars; Carruthers, Nicholas I.; Edwards, James P. published their research in Journal of Medicinal Chemistry on December 29 ,2005. The article was titled 《Preparation and Biological Evaluation of Indole, Benzimidazole, and Thienopyrrole Piperazine Carboxamides: Potent Human Histamine H4 Antagonists》.Product Details of 3584-66-5 The article contains the following contents:

Three series of H4 receptor ligands, derived from indoly-2-yl-(4-methyl-piperazin-1-yl)methanones, have been synthesized and their structure-activity relationships evaluated for activity at the H4 receptor in competitive binding and functional assays. In all cases, substitution of small lipophilic groups in the 4 and 5-positions led to increased activity in a [3H]histamine radiolabeled ligand competitive binding assay. In vitro metabolism and initial pharmacokinetic studies were performed on selected compounds leading to the identification of carboxamides I [X = CH, N] as potent H4 antagonists with the potential for further development. In addition, I demonstrated efficacy in in vitro mast cell and eosinophil chemotaxis assays. After reading the article, we found that the author used 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5Product Details of 3584-66-5)

5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5) belongs to imidazoles.Imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies.
However, the application of imidazoles is not limited to the field of peptides and peptidomimetics. Product Details of 3584-66-5

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Related Products of 3584-66-5On September 30, 2014 ,《Molecular properties prediction and synthesis of new benzimidazole H4-receptor antagonists as anti-inflammatory agents》 was published in Indian Journal of Heterocyclic Chemistry. The article was written by Bai, S. Anuradha; Tangeda, Sarita Jyostna; Madhavi, M.; Garlapati, Achaiah. The article contains the following contents:

The design and calculation of mol. properties, drug likeness, lipophilicity and solubility parameters of substituted benzimidazolyl carbonyl piperazines/piperidines I (R1 = Cl, CH3; R2 = H, Cl; R3 = CH3, C2H5; X = N, CH2) using mol inspiration, mol soft, software’s and ALOPGPS 2.1 program were investigated. Toxicity parameters were calculated using Osiris software. All compounds were non toxic; fulfill the solubility requirements and passing oral bioavailability criteria. Most of the compounds exhibited significant anti-inflammatory activity. In addition to this study using 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole, there are many other studies that have used 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5Related Products of 3584-66-5) was used in this study.

5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5) belongs to imidazoles.Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine. In addition, imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies. Related Products of 3584-66-5

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Recommanded Product: 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazoleOn November 1, 2004 ,《Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Terzioglu, Nalan; van Rijn, Richard M.; Bakker, Remko A.; De Esch, Iwan J. P.; Leurs, Rob. The article conveys some information:

The structure-activity relationship for a series of ligands structurally related to the recently identified (5-chloro-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone (I) as histamine H4 receptor (H4R) antagonists, is reported. Furthermore, related benzimidazoles was identified as lead compounds for the H4R. The ligands have been evaluated by radioligand displacement studies and functional assays for their interaction with both the human histamine H3 and H4 receptors and exhibit pKi values up to 7.5 at the human H4R. The experimental process involved the reaction of 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5Recommanded Product: 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole)

5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5) belongs to imidazoles.Imidazole rings are also present in imidazole ring alkaloids, which are potential therapeutics for thrombosis, cancer and inflammatory diseases.Recommanded Product: 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The author of 《Absorptimetric and fluorimetric study of solvent dependence and prototropism of 2-substituted benzimidazole derivatives》 were Sinha, Hemant K.; Dogra, Sneh K.. And the article was published in Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-1999) in 1987. Quality Control of 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole The author mentioned the following in the article:

A study of the effects of solvents on the absorption and fluorescence spectra of 2-substituted benzimidazoles showed that the lowest-energy transition of the chloromethyl, dichloromethyl, and cyanomethyl derivatives is of π-π* character, and that of the 5-chloro-2-(trichloromethyl), 2-(trifluoromethyl), and 2-chloro derivatives is of charge-transfer character. In the case of the monocations and monoanions of these compounds, the lowest-energy transitions are of charge-transfer and π-π* nature, resp. The presence of the methylene group between the benzimidazole and the heteroatom substituent reduces direct interaction; this is apparent from the study of proton-transfer reaction as well as from the spectral changes. The pKa values for these reactions in the ground and excited states were determined and discussed. MeCN quenches the fluorescence of the mono-, di-, and trichloromethyl compounds The mechanism could involve charge-transfer complexation.5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5Quality Control of 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole) was used in this study.

5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5) belongs to imidazoles.Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine. In addition, imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies. Quality Control of 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The author of 《Synthesis of novel histamine H4 receptor antagonists》 were Lane, Charlotte A. L.; Hay, Duncan; Mowbray, Charles E.; Paradowski, Michael; Selby, Matthew D.; Swain, Nigel A.; Williams, David H.. And the article was published in Bioorganic & Medicinal Chemistry Letters in 2012. Formula: C8H4Cl4N2 The author mentioned the following in the article:

This letter describes the discovery and synthesis of a series of octahydropyrrolo[3,4-c]pyrrole based selective histamine hH4 receptor antagonists. The amidine compound I was found to be a potent and selective histamine H4 receptor antagonist with moderate clearance and a high volume of distribution. The experimental process involved the reaction of 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5Formula: C8H4Cl4N2)

5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5) belongs to imidazoles.Imidazole rings are also present in imidazole ring alkaloids, which are potential therapeutics for thrombosis, cancer and inflammatory diseases.Formula: C8H4Cl4N2 Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Gupta, Radhey S. published an article on February 27 ,1987. The article was titled 《Identification of 2-benzimidazolylurea as a new antimitotic compound based on cross resistance studies with nocodazole resistant mutants of CHO cells》, and you may find the article in Biochemical and Biophysical Research Communications.Application In Synthesis of 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole The information in the text is summarized as follows:

The cross-resistance patterns of a set of nocodazole  [31430-18-9]-resistant (NocR) and podophyllotoxin  [518-28-5]-resistant (PodR) mutants of Chinese hamster ovary cells, which exhibit highly-specific cross-resistance toward compounds that show nocodazole-like antimitotic activity, towards a large number of benzimidazole derivatives was examined Of the various compounds examined, the NocR and the PodR mutants were found to exhibit increased cross-resistance towards only 2-benzimidazolylurea  [24370-25-0], indicating that this compound may possess similar biol. activity as nocodazole. The nocodazole-like antimitotic activity of 2-benzimidazolylurea was confirmed by its ability to block cells in mitosis, and by its competition of [3H]podophyllotoxin binding to microtubule proteins in cell extracts The nocodazole-like behavior of 2-benzimidazolylurea and lack of similar activity in other benzimidazole derivatives examined, provides valuable information regarding structural features that are required for this type of biol. activity. After reading the article, we found that the author used 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5Application In Synthesis of 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole)

5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5) belongs to imidazoles.Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine. Application In Synthesis of 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole In addition, imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

《2-(Trihalomethyl)benzazoles. I. Formation》 was published in Journal of the Chemical Society [Section] C: Organic in 1967. These research results belong to Holan, George; Samuel, Eva L.; Ennis, B. C.; Hinde, Ronald W.. Related Products of 3584-66-5 The article mentions the following:

Methods of preparation of 2-(trihalomethyl)benzimidazoles, -benzothiazoles, and -benzoxazoles were investigated. The reaction of the mono salts of o-phenylenediamines, o-aminophenols, and o-aminothiophenols with trichloroacetonitrile or trichloroacetimidate esters affords 2-(trichloromethyl)-substituted benzimidazoles, benzoaxazoles, and benzothiazoles. This method was extended to the preparation of 2-(trichloromethyl)-2-imidazolines. A general method of preparation of 2,2′-bibenzimidazolyl (I) derivatives is also described. 20 references. In the experiment, the researchers used 5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5Related Products of 3584-66-5)

5-Chloro-2-(trichloromethyl)-1H-benzo[d]imidazole(cas: 3584-66-5) belongs to imidazoles.Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine. Related Products of 3584-66-5 In addition, imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem