Category: 27469-61-0

COA of Formula: C17H18Cl2N2. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 1-(Bis(4-chlorophenyl)methyl)piperazine, is researched, Molecular C17H18Cl2N2, CAS is 27469-61-0, about Synthesis and antiallergic activities of diphenylmethylpiperazine derivatives. Author is Wang, Lisheng; Jiang, Hongyu; Zhou, Yonghong; Liu, Baili; Ji, Zhizhong.

The diphenylmethylpiperazine derivatives were designed and synthesized to find high anti-allergic compounds Twenty-one compounds of 1-R3-4-[(4-R1-phenyl)(4-R2-phenyl)methyl]piperazine (R1 = H, Cl, F, methoxy, tert-Bu, or nitro; R2 = H, F, Cl, or tert-butyl; and R3 = Et, benzyl, Bu, octyl, cetyl, or dodecyl), among which 17 compounds were new ones, were designed and synthesized from benzophenone derivatives by reduction with Zn/NaOH, substitution reaction with piperazine, and substitution reaction with R3Br. Their structures were identified by IR, 1H-NMR spectral, and elemental anal. Some compounds were evaluated from two pharmacol. models of the delayed-type hypersensitivity response to 2,4-dinitrochlorobenzene (DNCB) in mice and vascular permeability reduced by histamine in mice. Two compounds (R1 = R2 = H and R3 = Bu or dodecyl) had high antiallergic effects on the delayed-type hypersensitivity, and 5 compounds (R1 = R2 = H, R3 = octyl, cetyl, or dodecyl; R1 = nitro or F, R2 = H or F, R3 = dodecyl) had high antihistamine activity. Antiallergic activity was stronger with longer carbon chains.

There is still a lot of research devoted to this compound(SMILES：ClC1=CC=C(C=C1)C(N2CCNCC2)C3=CC=C(Cl)C=C3)COA of Formula: C17H18Cl2N2, and with the development of science, more effects of this compound(27469-61-0) can be discovered.

Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 1-(Bis(4-chlorophenyl)methyl)piperazine(SMILESS: ClC1=CC=C(C=C1)C(N2CCNCC2)C3=CC=C(Cl)C=C3,cas:27469-61-0) is researched.HPLC of Formula: 1452-77-3. The article 《Estrogen synthetase inhibitors. 2. Comparison of the in vitro aromatase inhibitory activity for a variety of nitrogen heterocycles substituted with diarylmethane or diarylmethanol groups》 in relation to this compound, is published in Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:27469-61-0).

The preparation and in vitro aromatase-inhibitory activity of a wide variety of heterocyclic diphenylmethane derivatives, e.g., (p-ClC4H4)2CRR1 (R = imidazolyl, pyridyl, pyrimidyl, etc.; R1 = H, HO, 1-imidazolyl), are described. Thus (p-ClC4H4)2CHCl was treated with imidazole in DMF containing NaH to give 1-[bis(p-chlorophenyl)methyl]imidazole. The choice of the 2 diaryl-bearing moieties as a vehicle for evaluating the heterocycles was made by comparing a series of imidazole- and pyridine-derived compounds with similar pyrimidine compounds reported previously. A structural model for the most active compounds is also presented. The activity of a related series of compounds containing 2 heterocyclic moieties was consistent with the model. Many of the compounds evaluated, including representatives of the pyridine, imidazole, pyrimidine, pyrazole, triazole, thiazole, and isothiazole classes, exhibit EC50 potencies for aromatase inhibition at low nanomolar levels. These compounds are at least as potent as other nonsteroidal aromatase inhibitors reported previously.

There is still a lot of research devoted to this compound(SMILES：ClC1=CC=C(C=C1)C(N2CCNCC2)C3=CC=C(Cl)C=C3)HPLC of Formula: 27469-61-0, and with the development of science, more effects of this compound(27469-61-0) can be discovered.

Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 1-(Bis(4-chlorophenyl)methyl)piperazine(SMILESS: ClC1=CC=C(C=C1)C(N2CCNCC2)C3=CC=C(Cl)C=C3,cas:27469-61-0) is researched.Recommanded Product: 58081-05-3. The article 《Synthesis and hypocholesterolemic activity of some N-diphenylmethylpiperazine derivatives》 in relation to this compound, is published in Archiv der Pharmazie (Weinheim, Germany). Let’s take a look at the latest research on this compound (cas:27469-61-0).

The synthesis and preliminary assays as hypocholesterolemic agents of five N-phenylmethylpiperazines I [ R = PhCC, 2-(2-thienyl)ethynyl, 2-(2-thienylvinyl); R1 = H, Cl] are described. Thus, 2-thienylacetylene was treated with 1-benphydrylpiperazine and HCHO to give 91% I (R = PhCC, R1 = Cl). The evaluations were carried out in hypercholesterolemic mice and two of these compounds were more effective than bezafibrate in the test employed. The di-p-chloro substituted compounds showed higher activity than their corresponding dechlorinated analogs.

If you want to learn more about this compound(1-(Bis(4-chlorophenyl)methyl)piperazine)Name: 1-(Bis(4-chlorophenyl)methyl)piperazine, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(27469-61-0).

Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-(Bis(4-chlorophenyl)methyl)piperazine( cas:27469-61-0 ) is researched.COA of Formula: C17H18Cl2N2.Eaton, John K.; Furst, Laura; Cai, Luke L.; Viswanathan, Vasanthi S.; Schreiber, Stuart L. published the article 《Structure-activity relationships of GPX4 inhibitor warheads》 about this compound( cas:27469-61-0 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: structure preparation GPX4 inhibitor propiolamide NO warhead; Covalent inhibitors; Ferroptosis; GPX4; Masked electrophiles. Let’s learn more about this compound (cas:27469-61-0).

Direct inhibition of GPX4 requires covalent modification of the active-site selenocysteine. While phenotypic screening has revealed that activated alkyl chlorides and masked nitrile oxides can inhibit GPX4 covalently, a systematic assessment of potential electrophilic warheads with the capacity to inhibit cellular GPX4 has been lacking. Here, we survey more than 25 electrophilic warheads across several distinct GPX4-targeting scaffolds. We find that electrophiles with attenuated reactivity compared to chloroacetamides are unable to inhibit GPX4 despite the expected nucleophilicity of the selenocysteine residue. However, highly reactive propiolamides we uncover in this study can substitute for chloroacetamide and nitroisoxazole warheads in GPX4 inhibitors. Our observations suggest that electrophile masking strategies, including those we describe for propiolamide- and nitrile-oxide-based warheads, may be promising for the development of improved covalent GPX4 inhibitors.

There is still a lot of research devoted to this compound(SMILES：ClC1=CC=C(C=C1)C(N2CCNCC2)C3=CC=C(Cl)C=C3)COA of Formula: C17H18Cl2N2, and with the development of science, more effects of this compound(27469-61-0) can be discovered.

Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

SDS of cas: 27469-61-0. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 1-(Bis(4-chlorophenyl)methyl)piperazine, is researched, Molecular C17H18Cl2N2, CAS is 27469-61-0, about Synthesis and in-vitro study of novel (Z)-1-benzhydryl-4-cinnamylpiperazine derivatives as potential anticancer agents. Author is Shivaprakash, S.; Kiran, K. R.; Diwakar, Latha; Reddy, G. Chandrasekara.

A series of novel (Z)-1-benzhydryl-4-cinnamylpiperazines I [R1 = R2 = Ph, 4-ClC6H4, 4-MeC6H4, 4-FC6H4; R1 = Ph, R2 = 4-ClC6H4, 4-BrC6H4; R3 = Ph, 4-MeOC6H4, 3,5-(MeO)2C6H3, piperonyl, etc.] was synthesized in six steps starting from the corresponding benzophenones R1COR2. The final step was Wittig condensation of the appropriate benzyltriphenylphosphonium halides R3CH2P+Ph3 X- (X = Cl, Br) with 1-benzhydryl-4-(formylmethyl)piperazines, which afforded pure (Z)-1-benzhydryl-4-cinnamylpiperazines I. The anticancer potential (MTT assay) of the synthesized compounds was tested against human cervical cancer (HeLa) and murine microglial (BV-2) cell lines. The compound I (R1 = R2 = 4-FC6H4; R3 = Ph) (cis-flunarizine) exhibited exceptionally superior activity against both HeLa and BV-2 cell lines with IC50 value of 13.23±3.51 μM and 23.1±4.12 μM, resp. Hence, this compound may be considered as a potential lead mol. for further development.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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. published the article 《Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection》. Keywords: chlorcyclizine hepatitis antiviral virus infection.They researched the compound: 1-(Bis(4-chlorophenyl)methyl)piperazine( cas:27469-61-0 ).Safety of 1-(Bis(4-chlorophenyl)methyl)piperazine. 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.

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.

If you want to learn more about this compound(1-(Bis(4-chlorophenyl)methyl)piperazine)Safety of 1-(Bis(4-chlorophenyl)methyl)piperazine, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(27469-61-0).

Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

SDS of cas: 27469-61-0. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 1-(Bis(4-chlorophenyl)methyl)piperazine, is researched, Molecular C17H18Cl2N2, CAS is 27469-61-0, about Molecular Shape and QSAR Analyses of a Family of Substituted Dichlorodiphenyl Aromatase Inhibitors. Author is Nagy, P. I.; Tokarski, John; Hopfinger, A. J..

Conformational analyses of three families of substituted dichlorodiphenyl aromatase inhibitors indicated that both potent and weak inhibitors adopt a common global min. energy conformation. Further, this global min. energy conformation is the only meaningful intramol. conformer state that can be energetically realized and is virtually identical to the crystal structure of one of the analogs. Quant. structure-activity relationships, QSARs, were sep., and jointly, developed for two series of inhibitors. The distance, D, of a nitrogen atom in the variable heterocyclefrom the core Cc atom is the most important activity descriptor. The optimum distance between the nitrogen and Cc to maximize inhibitor potency is about 3.6 Å for both classes of analogs. Integrated potential energy field difference calculations were also carried out using a proton probe and some of the variable heterocycles. The field calculations coupled with the QSAR studies suggest that the nitrogen 3.6 Å from Cc acts as a hydrogen bond acceptor. Two possible three-dimensional pharmacophores are proposed for effective aromatase inhibitors.

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Eaton, John K.; Furst, Laura; Cai, Luke L.; Viswanathan, Vasanthi S.; Schreiber, Stuart L. published the article 《Structure-activity relationships of GPX4 inhibitor warheads》. Keywords: structure preparation GPX4 inhibitor propiolamide NO warhead; Covalent inhibitors; Ferroptosis; GPX4; Masked electrophiles.They researched the compound: 1-(Bis(4-chlorophenyl)methyl)piperazine( cas:27469-61-0 ).Recommanded Product: 27469-61-0. 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.

Direct inhibition of GPX4 requires covalent modification of the active-site selenocysteine. While phenotypic screening has revealed that activated alkyl chlorides and masked nitrile oxides can inhibit GPX4 covalently, a systematic assessment of potential electrophilic warheads with the capacity to inhibit cellular GPX4 has been lacking. Here, we survey more than 25 electrophilic warheads across several distinct GPX4-targeting scaffolds. We find that electrophiles with attenuated reactivity compared to chloroacetamides are unable to inhibit GPX4 despite the expected nucleophilicity of the selenocysteine residue. However, highly reactive propiolamides we uncover in this study can substitute for chloroacetamide and nitroisoxazole warheads in GPX4 inhibitors. Our observations suggest that electrophile masking strategies, including those we describe for propiolamide- and nitrile-oxide-based warheads, may be promising for the development of improved covalent GPX4 inhibitors.

In some applications, this compound(27469-61-0)Recommanded Product: 27469-61-0 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 27469-61-0, is researched, SMILESS is ClC1=CC=C(C=C1)C(N2CCNCC2)C3=CC=C(Cl)C=C3, Molecular C17H18Cl2N2Journal, Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov’t, ACS Chemical Biology called Proteome-Wide Reactivity Profiling Identifies Diverse Carbamate Chemotypes Tuned for Serine Hydrolase Inhibition, Author is Chang, Jae Won; Cognetta, Armand B. III; Niphakis, Micah J.; Cravatt, Benjamin F., the main research direction is proteomewide reactivity profiling carbamate serine hydrolase monacylglyserol lipase.Formula: C17H18Cl2N2.

Serine hydrolases are one of the largest and most diverse enzyme classes in Nature. Inhibitors of serine hydrolases are used to treat many diseases, including obesity, diabetes, cognitive dementia, and bacterial and viral infections. Nonetheless, the majority of the 200+ serine hydrolases in mammals still lack selective inhibitors for their functional characterization. We and others have shown that activated carbamates, through covalent reaction with the conserved serine nucleophile of serine hydrolases, can serve as useful inhibitors for members of this enzyme family. The extent to which carbamates, however, cross-react with other protein classes remains mostly unexplored. Here, we address this problem by investigating the proteome-wide reactivity of a diverse set of activated carbamates in vitro and in vivo, using a combination of competitive and click chem. (CC)-activity-based protein profiling (ABPP). We identify multiple classes of carbamates, including O-aryl, O-hexafluoroisopropyl (HFIP), and O-N-hydroxysuccinimidyl (NHS) carbamates that react selectively with serine hydrolases across entire mouse tissue proteomes in vivo. We exploit the proteome-wide specificity of HFIP carbamates to create in situ imaging probes for the endocannabinoid hydrolases monoacylglycerol lipase (MAGL) and α-β hydrolase-6 (ABHD6). These findings, taken together, designate the carbamate as a privileged reactive group for serine hydrolases that can accommodate diverse structural modifications to produce inhibitors that display exceptional potency and selectivity across the mammalian proteome.

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《New derivatives of 1,4-disubstituted piperazine》. Authors are Morren, H. G.; Denayer, R.; Linz, R.; Mathieu, J.; Strubbe, H.; Trolin, S..The article about the compound:1-(Bis(4-chlorophenyl)methyl)piperazinecas:27469-61-0,SMILESS:ClC1=CC=C(C=C1)C(N2CCNCC2)C3=CC=C(Cl)C=C3).SDS of cas: 27469-61-0. Through the article, more information about this compound (cas:27469-61-0) is conveyed.

New 1,4-disubstituted piperazines were prepared and their tranquillizing properties and action on gastric ulcers examined ο-(Chlorobenzhydryl)piperazine with Me3N and PhCH2Cl in PhMe gave N-(ο-chlorobenzhydryl)-N’-benzylpiperazine, b0.005 210°; di-HCl salt, m. 223°. By refluxing 2 moles chloroethoxyethanol or chloroethoxyethoxyethanol with 110 g. Me3N and 1 mole of various substituted benzhydrylpiperazines the following N-(R1-substituted-benzhydryl)-N’-(R-substituted) piperazines were prepared (R’ = CH2CH2OCH2CH2OH) (R and b.p./mm. given): ο-Cl, 215°/0.01; p-Br, 224°/0.01; m-Cl, 215°/0.5; m-Br, 225°/0.02; ο-Br, 215-20°/0.1; m-OMe, 225°/ 0.07; m-Me, 210°/0.1; ο-C5H11O, 248°/0.01; m-Bu, 215°/0.01; ο-Me, 205°/0.01. (R = CH2CH2OCH2CH2OCH2CH2OH): m-Br, 240-5°/0.01; ο-Br, 240-5°/0.005; p-Br, 245-50°/0.02; ο-Cl, 240-5°/0.01. In an N atm. 0.1 g. atom Na is dissolved with warming in a convenient alc., after cooling 1-benzhydryl-4-(ω-chloroalkanoyl)piperazine in toluene added, the toluene distilled, the mixture heated 3 hrs at 140°, to the cooled liquid 3:7 EtOH-C6H6 added, the filtrate evaporated, and the residue distilled in vacuo. By this method the following N-(ο-chlorobenzhydryl)-N’-(R-substituted) piperazines were prepared (R and b.p./mm. given): CH2CH2O(CH2)5OH, 225°/0.003; CH2CH2OCH2CH(OH)CH2OH, 200°/0.05; CH2CH2OCH.(CH2)2.CH(OH). CH2.CH2, 260°/0.05. By refluxing 0.1 mole 1-(ο-chlorobenzhydryloxyethyl)piperazine with 0.11 mole triethylamine and 0.1 mole halogenated derivative, RX, in xylene 12 hrs. the following N-(ο-chlorobenzhydryloxyethyl)-N’-(R-substituted)piperazines were prepared (R and b.p./mm. given): Bu, 210°/0.1; (CH2)2OCH2CH2OH, 250°/0.03 (in the presence of excess chloroethoxyethanol); CH2Ph, 230-5°/0.1; ο-MeC6H4CH2, 234-6°/0.01; ο-ClC6H4CH2, 240°/0.1; ο-ClC6H4CO, 255°/0.1; p-Me3CC6H4CH2O(CH2)2, 245-50°/0.1. By refluxing 0.1 mole monosubstituted piperazine with 0.11 mole triethylamine and 0.1 mole of various appropriate ω-chloroalkanoyl and benzhydryl oxides in xylene during 12 hrs. the following N-[(R’-substituted)benzhydryloxyalkylene] – N’ – (R-substituted)piperazines (alkylene = (CH2)n) were prepared (R1, R, n, and b.p./mm. given): ο-Cl, H(I), 2, 193-5°/0.15; ο-Cl, Me, 2, 185-190°/0.1; ο-Cl, CHMe2, 2, 184-6°/0.04; ο-Me, CHMe2, 2, 170°/0.005; ο-Cl, CH2CHMe2, 2, 185-190°/0.02; ο-Cl, (cyclohexyl, 2, 235-40°/0.05; ο-Cl, 3-methylcyclohexyl, 2; 230-2°/0.01; H, CH2CH2OH, 2, 220°/0.1; ο-Cl, CH2CH(OH)CH2OH, 2, – (decompose); ο-Cl, ο-Me-C6H4CH2; 2; 235°/0.05; ο-Me, m-MeC6H4CH2, 2, 224°/0.015; m-Cl, m-MeC6H4CH2, 2, 250°/0.1; ο-Me, ο-MeC6H4CH2, 2, 215°/0.005; ο-Cl, CHMe2, 3, 215°/0.7; ο-Cl, m-MeC6H4CH2, 3, 250°/0.5; ο-Cl, ο-MeC6H4CH2, 3, 260°/0.1; ο-Cl, CHMe2, 4, 210°/0.1; ο-Cl, m-MeC6H4CH2, 4, 245°/0.1; ο-Cl, CHMe2, 6, 230°/0.2; ο-Cl, ο-MeC6H4CH2, 6, 265°/0.1. N-[2-(ο-Chlorobenzhydryloxy)ethyl]-N’-(2-hydroxyethyl)piperazine (II), b0.1 230°, was prepared in 65% yield by melting at 150° 1.1 mole N-hydroxy-N’-ethylpiperazine, adding dropwise 0.5 mole ο-ClC6H4CHClPh, and warming 2 hrs. at 150°. The mixture is cooled at 75° and 250 ml. C6H6 added. After cooling and addition of NaOH the benzene layer is washed, evaporated, and the residue distilled in vacuo. II (0.1 mole) and 0.11 mole NaNH2 in 100 ml. toluene is refluxed until no NH3 is liberated. After cooling at 30° 0.12 mole p-tert-butylbenzyl bromide is added and the mixture refluxed 2 hrs. The cooled mass is extracted with dilute HCl, the acid-extract basified with K2CO3, and extracted with C6H6. After evaporation the residue is distilled in vacuo, giving 45% N-[2-(ο-chlorobenzhydryloxy)ethyl] – N’- [2-(p-tert-butylbenzyloxy)ethyl]piperazine, b0.1 275°. By refluxing 0.1 mole I, 11 g. triethylamine, 100 ml. toluene, and 0.1 mole AcCl during 2 hrs. N-[2-(ο-chlorobenzhydryloxy)ethyl]-N’-acetylpiperazine (III) is formed, b0.02 220-5°. Reduction of III with LiAlH4 yielded 88% N-[2-(ο-chlorobenzhydryloxy)ethyl]-N’-ethylpiperazine, b0.03 178-80°.

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics