446.6292 | Heterocyclic Building Blocks-piperazine

Squires, Richard F. et al. published their research in Voprosy Meditsinskoi Khimii in 1997 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Quality Control of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide

Novel GABA_A receptor blockers: an attempt to find more potent clozapine-like selective GABA antagonists was written by Squires, Richard F.;Saederup, Else. And the article was included in Voprosy Meditsinskoi Khimii in 1997.Quality Control of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide This article mentions the following:

Because clozapine and a number of other antipsychotic, as well as antidepressant drugs selectively block subsets of GABA_A receptors, we have routinely screened 1100 compounds since 1983 for GABA antagonists effects on ³⁵S-TBPS binding, with a view to finding more potent clozapine-like selective GABA_A receptor blockers. About 225 GABA antagonists were identified. Among compounds not previously published, four groups of tricyclic compounds (phenothiazines, phenoxazines, acridines and phenazines) contained GABA_A receptor blockers, with acridines and oxidized phenothiazines in general being the most potent. Other active groups include cocaine derivatives, xanthines, indoles and phenethylamine derivatives A large group of miscellaneous structures includes all known GABA_A receptor blockers, as well as some antihistamines, antitussives, antimalarial/antiprotozoals, potential antidepressant, and a large non-therapeutic category consisting of diverse chem. structures. The amidino steroid R5135 remains the most potent GABA_A receptor blocker by far (EC₅₀ = 5.7 nM, ΔB_opt = 130%), and is non-aromatic Pitrazepin, the next-most potent GABA_A receptor blocker (EC₅₀ = 360 nM), also fully reverses the inhibitory effect of 1 μM GABA on ³⁵S-TBPS binding, but is 63-fold less potent than R5135. Appropriately positioned amidino groups, ring (aromatic) nitrogen, ether and keto groups can contribute to the potency of GABA_A receptor blockade. Clozapine-like selective GABA_A receptor blockers with EC₅₀ values in the low nanomolar range remain to be identified. Such compounds may have potent antipsychotic effects. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Quality Control of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide).

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Tsakovska, Ivanka M. et al. published their research in Bioorganic & Medicinal Chemistry in 2003 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Recommanded Product: N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide

QSAR and 3D-QSAR of phenothiazine type multidrug resistance modulators in P388/ADR cells was written by Tsakovska, Ivanka M.. And the article was included in Bioorganic & Medicinal Chemistry in 2003.Recommanded Product: N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide This article mentions the following:

A series of 25 phenothiazines and structurally related compounds was investigated by QSAR (quant. structure activity relationship) and 3D-QSAR methods with respect to their MDR (multidrug resistance) reversing activity in P388/ADR- murine leukemia cell line resistant to ADR (adriamycin). The objective was to outline structural properties important for the investigated activity. Different measures for MDR reversal were used and compared. Two 3D-QSAR approaches were applied-CoMFA (comparative mol. field anal.) and CoMSIA (comparative mol. similarity indexes anal.). Both, neutral and protonated forms of the compounds were investigated. Mol. models with good predictive power were derived using a hydrophobic field alone and a combination of steric, hydrophobic, and hydrogen bond acceptor fields of the compounds In the combined models highest contribution of the hydrogen bond acceptor field was noticed. Thus, the dominant role of the hydrophobic and hydrogen bond acceptor fields for MDR reversing activity of the investigated compounds was demonstrated. The structural regions responsible for the differences in anti-MDR activity were analyzed in respect to their hydrophobic, hydrogen bond acceptor and steric nature. The results may direct design of new phenothiazines and related compounds as MDR modulators. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Recommanded Product: N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide).

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Robinson, Katherine et al. published their research in Journal of Immunoassay in 1985 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Application In Synthesis of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide

Radioimmunoassay of tricyclic antidepressant and some phenothiazine drugs in forensic toxicology was written by Robinson, Katherine;Smith, R. N.. And the article was included in Journal of Immunoassay in 1985.Application In Synthesis of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide This article mentions the following:

A RIA for screening blood and urine for tricyclic antidepressant and some phenothiazine drugs in forensic toxicol. is described. The assay has a broad cross-reactivity that enables therapeutic or subtherapeutic levels of most tricyclic antidepressants and a number of phenothiazines in blood to be detected. The antiserum is com. available and the radioligand, a radioiodinated conjugate of N-acetyl-L-histidine and nortriptyline聽聽[72-69-5], are easily prepared Blood samples required prior extraction to reduce the background but urine may be assayed directly. Seventy five 渭L of blood or 100 渭L of urine are required. Hemolysis or decomposition of the samples, common anticoagulants, and NaF do not affect the results. Data for 57 compounds are presented. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Application In Synthesis of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide).

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Turcant, A. et al. published their research in Clinical Chemistry (Washington, DC, United States) in 1991 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Computed Properties of C22H30N4O2S2

Toxicological screening of drugs by microbore high-performance liquid chromatography with photodiode-array detection and ultraviolet spectral library searches was written by Turcant, A.;Premel-Cabic, A.;Cailleux, A.;Allain, P.. And the article was included in Clinical Chemistry (Washington, DC, United States) in 1991.Computed Properties of C22H30N4O2S2 This article mentions the following:

UV data, acquired with a photodiode-array detector coupled to a reversed-phase liquid-chromatog. system, was used to identify unknown drugs in plasma samples of acutely poisoned patients. Both retention time and spectra of the peaks obtained with a microbore Hypersil ODS column under gradient elution are compared with a library of 鈭?50 compounds The authors three-year experience with this system, which identifies drugs in <1 h, with a high degree of confidence is presented. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Computed Properties of C22H30N4O2S2).

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Barbato, Francesco et al. published their research in European Journal of Medicinal Chemistry in 1982 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Category: piperazines

Hydrophobic constants and quantitative structure activity relationships (QSAR) in sets of phenothiazine drugs was written by Barbato, Francesco;Recanatini, Maurizio;Silippo, Carlo;Vittoria, Antonio. And the article was included in European Journal of Medicinal Chemistry in 1982.Category: piperazines This article mentions the following:

Octanol/water partition coefficients of a large set of phenothiazine drugs I [R = Me₂N(CH₂)₃, CH₂CHMeNMe₂, CH₂CHMeCH₂NMe₂, etc.; R¹ = H, Cl, CN, Me, CF₃, etc.] were determined and related to the corresponding high-performance liquid chromatog. capacity factors. The bovine serum albumin binding affinity and antihemolytic activity of sets of congeners are discussed from the quant. structure-activity point of view. Results show that both activities are largely affected by the degree of hydrophobicity of the mols. as measured by the log P apparent values, while other factors play only a minor role. Moreover, in vivo data are considered to uncover quant. correlations between structural features and neuroleptic biol. activities. Correlation equations show that the major factor influencing the considered activities is a particular electronic demand of the phenothiazine side chain, while 2-R¹-substituents may enhance the activity either affecting the side chain conformation or directly interacting at receptor site. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Category: piperazines).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Basavaiah, K. et al. published their research in Eastern Pharmacist in 1998 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Safety of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide

Determination of some phenothiazine neuroleptics by means of absorption spectrophotometry was written by Basavaiah, K.;Krishnamurthy, G.;Swamy, J. Manjunatha. And the article was included in Eastern Pharmacist in 1998.Safety of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide This article mentions the following:

A simple, rapid and sensitive spectrophotometric method was described for the quant. determination of 6 phenothiazine-based antipsychotic and anticholinergic drugs in bulk and in formulations. The method is based on the formation of stable phenothiazinium free radical cation by the use of sodium nitroprusside as the chromogenic agent. The drugs in a 1.5-2.5M H₂SO₄ medium reacted with the reagent to give intense orange or purple products which had characteristic absorption maxima at 500-530 nm. Beer’s law was obeyed over the concentration range 4-32 渭g/mL with apparent molar absorptivities ranging from 9.8 脳 10³ 16.59 脳 103 l.mol.^-1 cm^-1. The average percent recovery was 99.5-101.6. The accuracy and precision of the assay method were comparable to those of the British Pharmacopeia method. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Safety of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide).

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Ishikawa, Yasunobu et al. published their research in Forensic Science International in 1990 | CAS: 316-81-4

Positive- and negative-ion mass spectrometry and rapid clean-up of 19 phenothiazines was written by Ishikawa, Yasunobu;Suzuki, Osamu;Hattori, Hideki. And the article was included in Forensic Science International in 1990.Product Details of 316-81-4 This article mentions the following:

Pos.-ion electron impact (PIEI), pos.-ion chem. ionization (PICI), and neg.-ion chem. ionization (NICI) mass spectra of 19 phenothiazines are presented. In the PIEI mode, peaks due to M, M minus side chain (M – R₁), M – R₁ + H, and side chain itself (R₁) appeared for most compounds The M – R₁ ions were very useful for drug screening. In the PICI mode, most spectra showed base or intense peaks due to M + H, and small peaks due to M + C₂H₅; peaks due to M – R₁ also appeared in many compounds In the NICI mode, fragmentation modes were different in different compound groups; mol. or [M – H]^– quasimol. anions appeared in many compounds with aliphatic side chains. Anions at m/z 98 and 115 were characteristic for compounds with (N-methylpiperazinyl)propyl side chains. Selected ion monitoring in the PIEI mode generally gave much higher sensitivity than in the PICI and NICI modes. Phenothiazines present in urine or plasma could be rapidly isolated by use of Sep-Pak C₁₈ cartridges. Thirteen of 19 phenothaizines could be detected by HP-17 wide-bore capillary gas chromatog. with satisfactory separation from impurities in their underivatized forms. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Product Details of 316-81-4).

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Quinones-Torrelo, C. et al. published their research in Biomedical Chromatography in 2001 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Computed Properties of C22H30N4O2S2

An LD₅₀ model for predicting psychotropic drug toxicity using biopartitioning micellar chromatography was written by Quinones-Torrelo, C.;Sagrado-Vives, S.;Villanueva-Camanas, R. M.;Medina-Hernandez, M. J.. And the article was included in Biomedical Chromatography in 2001.Computed Properties of C22H30N4O2S2 This article mentions the following:

The LD₅₀ determination is the main way to measure the acute toxicity of all types of substances. At the present time, however, there is increasing opposition to the use of living animals in research and testing activities from animal rights groups as well as some scientists. Nevertheless, the need to have a tool for estimating the potential toxicity of new compounds for human consumption has encouraged the development of alternative methods. Under adequate conditions, the partitioning in micellar liquid chromatog. can describe the drug biopartitioning. We have named this chromatog. system biopartitioning micellar chromatog. (BMC). In this paper, an LD₅₀ QRAR model developed for psychotropic drugs from their retention data in BMC, is described. The model’s ability to predict new psychotropic drug toxicity is statistically proved. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Computed Properties of C22H30N4O2S2).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Computed Properties of C22H30N4O2S2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Revanasiddappa, H.D. et al. published their research in Eastern Pharmacist in 1995 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Related Products of 316-81-4

Spectrophotometric determination of some phenothiazine derivatives in pharmaceutical preparations was written by Revanasiddappa, H.D.;Ramappa, P.G.. And the article was included in Eastern Pharmacist in 1995.Related Products of 316-81-4 This article mentions the following:

A simple, accurate and rapid method for the quant. determination of phenothiazine drugs in either the bulk or in pharmaceuticals is based on the development of colored compounds with vanadoboric acid in acid medium. The reaction is suggested to proceed via oxidation of the phenothiazine nucleus into a semiquinonoid radical. A study of the effect of commonly associated excipients revealed that they did not cause any interference. Statistical anal. of results indicates that the method is precise and accurate. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Related Products of 316-81-4).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Related Products of 316-81-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Hayano, Taizo et al. published their research in Wakayama Igaku in 2005 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Synthetic Route of C22H30N4O2S2

Characteristics of drugs evaluated by computational chemistry. (5). Typical antipsychotics was written by Hayano, Taizo;Kishioka, Shiroh;Yamamoto, Hiroyuki;Ikoma, Yoshihisa. And the article was included in Wakayama Igaku in 2005.Synthetic Route of C22H30N4O2S2 This article mentions the following:

Antipsychotics are divided into two types, i.e. typical type and atypical type. Typical type mainly includes phenothiazines and butyrophenones. Risperidone is located on the boundary. We furthermore divide the typical type into umbrella shape and cylindrical shape based on the mol. form. They have the side chain that connect with main ring with characteristic bond angle. Electron d. was high on main ring where HOMO and LUMO localized and low on terminal chain. Statistical anal. showed that there are no significant difference on the electron energies, the dipole moments, the dihedral angles between umbrella shape mols. and cylindrical ones. These results suggested the importance of the Pr group joining to the side chain with main ring. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Synthetic Route of C22H30N4O2S2).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Synthetic Route of C22H30N4O2S2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics