Category: 27469-61-0

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Development of small-molecule probes that selectively kill cells induced to express mutant RAS, published in 2012-02-15, which mentions a compound: 27469-61-0, Name is 1-(Bis(4-chlorophenyl)methyl)piperazine, Molecular C17H18Cl2N2, Category: tetrahydropyran.

Synthetic lethal screening is a chem. biol. approach to identify small mols. that selectively kill oncogene-expressing cell lines with the goal of identifying pathways that provide specific targets against cancer cells. We performed a high-throughput screen of 303,282 compounds from the National Institutes of Health-Mol. Libraries Small Mol. Repository (NIH-MLSMR) against immortalized BJ fibroblasts expressing HRASG12V followed by a counterscreen of lethal compounds in a series of isogenic cells lacking the HRASG12V oncogene. This effort led to the identification of two novel mol. probes (PubChem CID 3689413, ML162 and CID 49766530, ML210) with nanomolar potencies and 4-23-fold selectivities, which can potentially be used for identifying oncogene-specific pathways and targets in cancer cells.

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Song, Kwang-Seop; Lee, Sung-Han; Chun, Hyun Ji; Kim, Jong Yup; Jung, Myung Eun; Ahn, Kwangwoo; Kim, Soo-Un; Kim, Jeongmin; Lee, Jinhwa published the article 《Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands》. Keywords: CB1 cannabinoid antagonist piperazine preparation SAR.They researched the compound: 1-(Bis(4-chlorophenyl)methyl)piperazine( cas:27469-61-0 ).Formula: C17H18Cl2N2. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:27469-61-0) here.

After the CB1 receptor antagonist SR141716 (rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. Several series of urea, carbamate, amide, sulfonamide and oxalamide derivatives based on 1-benzhydrylpiperazine scaffold were synthesized and tested for CB1 receptor binding affinity. The SAR studies to optimize the CB1 binding affinity led to the potent urea derivatives After the addnl. SAR studies to optimize the substituents of di-Ph rings, the combination of 2-chlorophenyl and 4-chlorophenyl turned out to be the most potent scaffold. The CB2 binding affinity assay as well as functional assay was also conducted on these compounds Herein we wish to introduce several novel CB1 antagonists with IC50 values less than 100 nM for the CB1 receptor binding.

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Tetrahydropyran – Wikipedia,
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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Dhainaut, Alain; Regnier, Gilbert; Atassi, Ghanem; Pierre, Alain; Leonce, Stephane; Kraus-Berthier, Laurence; Prost, Jean Francois researched the compound: 1-(Bis(4-chlorophenyl)methyl)piperazine( cas:27469-61-0 ).Recommanded Product: 27469-61-0.They published the article 《New triazine derivatives as potent modulators of multidrug resistance》 about this compound( cas:27469-61-0 ) in Journal of Medicinal Chemistry. Keywords: triazine modulator multidrug resistance; cytotoxic agent modulator multidrug resistance triazine; structure activity multidrug resistance modulator triazine. We’ll tell you more about this compound (cas:27469-61-0).

70 Triazines, e.g., I (X = bond, NH, aminoalkylene; Y = N; R = diarylalkyl, dibenzocycloheptenyl, dibenzoheteroaryl) were prepared from chlorotrazines and tested for their capacity to modulate multidrug resistance (MDR) in DC-3F/AD and KB-A1 tumor cells in vitro, in comparison with verapamil (VRP), a calcium channel antagonist currently used in therapy as an antihypertensive drug, which also shows MDR modulating activity. Among the 12 selected compounds, I [X = bond, Y = CH, R = NHCH2CH(C6H4F-4)2] (II) (S9788) showed high MDR reversing properties in vitro (300- and 6-fold VRP at 5 μM in DC-3F/AD and KB-A1 cells, resp.) and induced a strong accumulation of adriamycin. The relationship between the increase of ADR accumulation and the fold reversal induced by these compounds and their lack of effects on the sensitive DC-3F cells suggest that they act mainly by inhibiting the Pgp-catalyzed efflux of cytotoxic agents, as already described for a majority of MDR modulators. In vivo, in association with the antitumor drug vincristine (0.25 mg/kg), II (100 mg/kg) increased the T/C by 39% in mice bearing the resistant tumor cell line P388/VCR. According to these interesting properties, II was selected for a clin. development because it was more bioavailable than I [X = bond, Y = CH, R = (dibenzo[a,d]cyclohepten-5-ylmethyl)amino] , even though it was less active.

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Tetrahydropyran – an overview | ScienceDirect Topics

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamides, published in 1989-03-31, which mentions a compound: 27469-61-0, Name is 1-(Bis(4-chlorophenyl)methyl)piperazine, Molecular C17H18Cl2N2, Safety of 1-(Bis(4-chlorophenyl)methyl)piperazine.

A new series of 3-(3-pyridyl)acrylamides, e.g., I (R = H, R1 = 4-F, 4-Cl, 4-OMe, 3-Me, 4-Me, R2 = H, 4-Cl, 4-Me; R = 2-Cl, 2-NHMe, 2-Me, 5-F, 5-Cl, 5-Br, 5-OMe, 5-OH, 6-Cl, 6-OMe, 6-Me, 6-Bu, R1 = R2 = H), and 5-(3-pyridyl)-2,4-pentadienamides, e.g., II (R = H, Me, n = 3,4) were prepared and evaluated for antiallergic activity. Several of these compounds exhibited more potent inhibitory activities than the parent compound I (R = R1 = R2 = H) against the rat passive cutaneous anaphylaxis (PCA) reaction and the enzyme 5-lipoxygenase. Particularly, I (R = 6-Me, R1 = R2 = H) (III) showed an ED50 value of 3.3 mg/kg po in the rat PCA test, which was one-fifth of ketotifen and oxatomide. As compared with ketotifen and oxatomide, III showed a better balance of antiallergic properties due to inhibition of chem. mediator release, inhibition of 5-lipoxygenase, and antagonism of histamine.

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Formula: C17H18Cl2N2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 1-(Bis(4-chlorophenyl)methyl)piperazine, is researched, Molecular C17H18Cl2N2, CAS is 27469-61-0, about Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection. Author is He, Shanshan; Xiao, Jingbo; Dulcey, Andres E.; Lin, Billy; Rolt, Adam; Hu, Zongyi; Hu, Xin; Wang, Amy Q.; Xu, Xin; Southall, Noel; Ferrer, Marc; Zheng, Wei; Liang, T. Jake; Marugan, Juan J..

Recently, we reported that chlorcyclizine (CCZ, Rac-2), an over-the-counter antihistamine piperazine drug, possesses in vitro and in vivo activity against hepatitis C virus. Here, we describe structure-activity relationship (SAR) efforts that resulted in the optimization of novel chlorcyclizine derivatives as anti-HCV agents. Several compounds exhibited EC50 values below 10 nM against HCV infection, cytotoxicity selectivity indexes above 2000, and showed improved in vivo pharmacokinetic properties. The optimized mols. can serve as lead preclin. candidates for the treatment of hepatitis C virus infection and as probes to study hepatitis C virus pathogenesis and host-virus interaction.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Quality Control of 1-(Bis(4-chlorophenyl)methyl)piperazine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 1-(Bis(4-chlorophenyl)methyl)piperazine, is researched, Molecular C17H18Cl2N2, CAS is 27469-61-0, about Synthesis and pharmacological study of new calcium antagonists, analogs of cinnarizine and flunarizine. Author is Younes, S.; Baziard-Mouysset, G.; de Saqui-Sannes, G.; Stigliani, J. L.; Payard, M.; Bonnafous, R.; Tisne-Versailles, J..

Several phosphonic di-Et esters were prepared and their Ca antagonistic activity evaluated in vitro. The di-Et phosphonate group was condensed on substituted [diphenylmethyl], [(2-benzofuranyl)phenylmethyl], [(4-diphenylmethyl-1-piperazinyl) methyl], [4-(4-diphenylmethyl-1-piperazinyl methyl) phenylmethyl], and [4-(3-phenyl-2-propenyl)-1-piperazinyl methyl] groups. Despite the presence of the di-Et phosphonate moiety and the benzhydrylpiperazinyl group, both present in potent Ca antagonist structures, only one of the 19 prepared compounds, i.e. I, exhibited a Ca antagonistic profile.

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Tetrahydropyran – an overview | ScienceDirect Topics

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Development and validation of an in silico P450 profiler based on pharmacophore models, published in 2006-03-31, which mentions a compound: 27469-61-0, mainly applied to Cytochrome P450 inhibitor pharmacophore model enzyme kinetics, Electric Literature of C17H18Cl2N2.

In today’s drug discovery process, the very early consideration of ADME properties is aimed at a reduction of drug candidate drop out rate in later development stages. A part from in vitro testing, in silico methods are evaluated as complementary screening tools for compounds with unfavorable ADME attributes. Especially members of the cytochrome P 450 (P 450) enzyme superfamily. e.g. P 450 1A2, P 450 2C9, P 450 2C19, P 450 2D6, and P 450 3A4, contribute to xenobiotic metabolism, and compound interaction with one of these enzymes is therefore critically evaluated. Pharmacophore models are widely used to identify common features amongst ligands for any target. In this study, both structure-based and ligand-based models for prominent drug-metabolizing members of the P 450 family were generated employing the software packages LigandScout and Catalyst. Essential chem. ligand features for substrate and inhibitor activity for all five P 450 enzymes investigated were determined and analyzed. Finally, a collection of 11 pharmacophores for substrates and inhibitors was evaluated as an in silico P 450 profiling tool that could be used for early ADME estimation of new chem. entities.

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, N.I.H., Extramural, Research Support, N.I.H., Intramural, Journal of Medicinal Chemistry called Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection, Author is He, Shanshan; Xiao, Jingbo; Dulcey, Andres E.; Lin, Billy; Rolt, Adam; Hu, Zongyi; Hu, Xin; Wang, Amy Q.; Xu, Xin; Southall, Noel; Ferrer, Marc; Zheng, Wei; Liang, T. Jake; Marugan, Juan J., which mentions a compound: 27469-61-0, SMILESS is ClC1=CC=C(C=C1)C(N2CCNCC2)C3=CC=C(Cl)C=C3, Molecular C17H18Cl2N2, Formula: C17H18Cl2N2.

Recently, we reported that chlorcyclizine (CCZ, Rac-2), an over-the-counter antihistamine piperazine drug, possesses in vitro and in vivo activity against hepatitis C virus. Here, we describe structure-activity relationship (SAR) efforts that resulted in the optimization of novel chlorcyclizine derivatives as anti-HCV agents. Several compounds exhibited EC50 values below 10 nM against HCV infection, cytotoxicity selectivity indexes above 2000, and showed improved in vivo pharmacokinetic properties. The optimized mols. can serve as lead preclin. candidates for the treatment of hepatitis C virus infection and as probes to study hepatitis C virus pathogenesis and host-virus interaction.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Dhainaut, Alain; Regnier, Gilbert; Atassi, Ghanem; Pierre, Alain; Leonce, Stephane; Kraus-Berthier, Laurence; Prost, Jean Francois published an article about the compound: 1-(Bis(4-chlorophenyl)methyl)piperazine( cas:27469-61-0,SMILESS:ClC1=CC=C(C=C1)C(N2CCNCC2)C3=CC=C(Cl)C=C3 ).HPLC of Formula: 27469-61-0. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:27469-61-0) through the article.

70 Triazines, e.g., I (X = bond, NH, aminoalkylene; Y = N; R = diarylalkyl, dibenzocycloheptenyl, dibenzoheteroaryl) were prepared from chlorotrazines and tested for their capacity to modulate multidrug resistance (MDR) in DC-3F/AD and KB-A1 tumor cells in vitro, in comparison with verapamil (VRP), a calcium channel antagonist currently used in therapy as an antihypertensive drug, which also shows MDR modulating activity. Among the 12 selected compounds, I [X = bond, Y = CH, R = NHCH2CH(C6H4F-4)2] (II) (S9788) showed high MDR reversing properties in vitro (300- and 6-fold VRP at 5 μM in DC-3F/AD and KB-A1 cells, resp.) and induced a strong accumulation of adriamycin. The relationship between the increase of ADR accumulation and the fold reversal induced by these compounds and their lack of effects on the sensitive DC-3F cells suggest that they act mainly by inhibiting the Pgp-catalyzed efflux of cytotoxic agents, as already described for a majority of MDR modulators. In vivo, in association with the antitumor drug vincristine (0.25 mg/kg), II (100 mg/kg) increased the T/C by 39% in mice bearing the resistant tumor cell line P388/VCR. According to these interesting properties, II was selected for a clin. development because it was more bioavailable than I [X = bond, Y = CH, R = (dibenzo[a,d]cyclohepten-5-ylmethyl)amino] , even though it was less active.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Reference of 1-(Bis(4-chlorophenyl)methyl)piperazine. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 1-(Bis(4-chlorophenyl)methyl)piperazine, is researched, Molecular C17H18Cl2N2, CAS is 27469-61-0, about Design, Synthesis, and Biological Evaluation of 2-((4-Bisarylmethyl-piperazin-1-yl)methyl)benzonitrile Derivatives as HCV Entry Inhibitors. Author is Wang, Yixuan; Li, Jianrui; Tan, Jiali; Yang, Bo; Quan, Yanni; Peng, Zonggen; Li, Yanping; Li, Zhuorong.

Viral entry inhibitors are absent in hepatitis C virus (HCV) treatment regimens although a dozen direct-acting antiviral (DAA) drugs are available now. Based on a previously identified HCV entry inhibitor L0909, chem. space exploration and structure-activity relationship (SAR) studies led to the discovery of a new derived scaffold 2-((4-bisarylmethyl-piperazin-1-yl)methyl)benzonitrile. Several new scaffold derivatives exhibited higher in vitro anti-HCV activity at low nanomolar concentrations compared to L0909. A biol. study indicated that the high potency of few active derivatives were primarily driven by the inhibitory effect on the virus entry stage. Moreover, an SPR experiment confirmed that this class of derivatives might target the HCV E1 protein. Pharmacokinetic studies indicated that few compounds are orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. In conclusion, this work provided a novel 2-((4-bisarylmethyl-piperazin-1-yl)methyl)benzonitrile chemotype deserving further investigation into its antiviral therapeutic potential.

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