Category: piperazines

Utility of Gold Nanoparticles for Spectrofluorimetric and Spectrophotometric Determination of Sildenafil Citrate, Dapoxetine, Vardenafil and Tadalafil in their Dosage Forms and Biological Fluids was written by Salem, Hesham;Abdel Aziz, Basma E.. And the article was included in Analytical Chemistry Letters in 2020.Electric Literature of C23H32N6O4S This article mentions the following:

Two simple, rapid and novel sensitive fluorimetric and spectrophotometric methods were investigated for the assay of sildenafil citrate (SIL), dapoxetine (DAP), vardenafil (VAD) and tadalafil (TAD) using gold nanoparticles (Au NPs). On the spectrofluorimetric method, gold nanoparticles were used as a fluorescence probe. The addition of drugs to Au-NPs solution caused considerable quenching of the emission band of Au-NPs, which was likely due to the complexation of the drug to gold NPs. Under the optimum conditions, the quenched fluorescence (FL) intensity was linear with the studied concentrations The quenching mechanism of the studied drugs on the emission band of Au-NPs was explained by Stern-Volmer law. The second spectrophotometric method was based on aggregation of synthesized gold nanoparticles. Gold nanoparticles showed absorption at 522 nm. Upon interaction with the cited drugs, the band at 522 nm disappeared with the formation of a new red-shifted band at 673, 660, 665, and 663 nm for SIL, TAD, VAD, and DAP, resp. Different exptl. factors were optimized for higher sensitivity. The calibration curves were linear with a concentration range of 0.1-12 μg/mL for the studied drugs. The methods were applied successfully to determine the studied drugs in minor concentrations in pure form, pharmaceutical dosage forms, and biol. fluids (human serum and urine). In the experiment, the researchers used many compounds, for example, 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4Electric Literature of C23H32N6O4S).

2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4) 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. Electric Literature of C23H32N6O4S

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

Association between sexual activity-related death and non-prescription use of phosphodiesterase type 5 inhibitors was written by Nagasawa, Sayaka;Saka, Kanju;Yamagishi, Yoshikazu;Yajima, Daisuke;Chiba, Fumiko;Yamaguchi, Rutsuko;Torimitsu, Suguru;Iwase, Hirotaro. And the article was included in Legal Medicine in 2021.Related Products of 224785-90-4 This article mentions the following:

In recent years, there has been an increase in the use of phosphodiesterase type 5 inhibitors (PDE5i) that are purchased from abroad without a doctor’s diagnosis via the Internet or other means. We report six cases in which nonprescription use of PDE5i may have led to death. Among the four deceased individuals who were believed to have experienced sudden cardiac death, three (cases 1-3) had a history of cardiovascular disease, which is a contraindication, and the remaining case (case 4) involved combined use of multiple PDE5i. Sildenafil (0.063μg/mL, 0.087μg/mL) was detected in two of the four cases of sudden cardiac death. Tadalafil (0.096μg/mL) was detected in one of the remaining two cases, and tadalafil (0.197μg/mL) and vardenafil (0.011μg/mL) were detected in the other case. Sildenafil (0.032μg/mL), tadalafil (0.062μg/mL), and ethanol were detected in a traffic accident case with a history of contraindications. In a case of asphyxiation by vomit aspiration, autopsy showed 90% stenosis in the anterior descending branch of the coronary artery, and sildenafil (0.063μg/mL) was detected. To the best of our knowledge, this is the first report of postmortem blood levels of tadalafil and vardenafil likely contributing to the cause of death. Despite all the warnings about the dangers of using PDE5 inhibitors, cases of PDE5i contributing to death are still identified during autopsies. Therefore, raising public awareness of the risks of the risks associated with the imported drug use by individuals is necessary. In the experiment, the researchers used many compounds, for example, 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4Related Products of 224785-90-4).

2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4) 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.Related Products of 224785-90-4

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

Pd-PEPPSI-IPent: Low-Temperature Negishi Cross-Coupling for the Preparation of Highly Functionalized, Tetra-ortho-Substituted Biaryls was written by Calimsiz, Selcuk;Sayah, Mahmoud;Mallik, Debasis;Organ, Michael G.. And the article was included in Angewandte Chemie, International Edition in 2010.HPLC of Formula: 331767-56-7 This article mentions the following:

Pd-PEPPSI-IPent catalyzed the Negishi cross-coupling reactions of arylzinc halides with aryl/heteroaryl bromides or chlorides for the synthesis of very challenging and structurally diverse biaryl compounds In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(6-bromopyridin-2-yl)piperazine-1-carboxylate (cas: 331767-56-7HPLC of Formula: 331767-56-7).

tert-Butyl 4-(6-bromopyridin-2-yl)piperazine-1-carboxylate (cas: 331767-56-7) 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 is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.HPLC of Formula: 331767-56-7

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

TP-0903 is active in models of drug-resistant acute myeloid leukemia. was written by Jeon, Jae Yoon;Buelow, Daelynn R;Garrison, Dominique A;Niu, Mingshan;Eisenmann, Eric D;Huang, Kevin M;Zavorka Thomas, Megan E;Weber, Robert H;Whatcott, Clifford J;Warner, Steve L;Orwick, Shelley J;Carmichael, Bridget;Stahl, Emily;Brinton, Lindsey T;Lapalombella, Rosa;Blachly, James S;Hertlein, Erin;Byrd, John C;Bhatnagar, Bhavana;Baker, Sharyn D. And the article was included in JCI insight in 2020.Application of 1341200-45-0 This article mentions the following:

Effective treatment for AML is challenging due to the presence of clonal heterogeneity and the evolution of polyclonal drug resistance. Here, we report that TP-0903 has potent activity against protein kinases related to STAT, AKT, and ERK signaling, as well as cell cycle regulators in biochemical and cellular assays. In vitro and in vivo, TP-0903 was active in multiple models of drug-resistant FLT3 mutant AML, including those involving the F691L gatekeeper mutation and bone marrow microenvironment-mediated factors. Furthermore, TP-0903 demonstrated preclinical activity in AML models with FLT3-ITD and common co-occurring mutations in IDH2 and NRAS genes. We also showed that TP-0903 had ex vivo activity in primary AML cells with recurrent mutations including MLL-PTD, ASXL1, SRSF2, and WT1, which are associated with poor prognosis or promote clinical resistance to AML-directed therapies. Our preclinical studies demonstrate that TP-0903 is a multikinase inhibitor with potent activity against multiple drug-resistant models of AML that will have an immediate clinical impact in a heterogeneous disease like AML. In the experiment, the researchers used many compounds, for example, 2-((5-Chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide (cas: 1341200-45-0Application of 1341200-45-0).

2-((5-Chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide (cas: 1341200-45-0) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. 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.Application of 1341200-45-0

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

Synthesis and antioxidant activity of some 1-aryl/aralkyl piperazine derivatives with xanthine moiety at N4 was written by Andonova, Lily;Zheleva-Dimitrova, Dimitrina;Georgieva, Maya;Zlatkov, Alexander. And the article was included in Biotechnology & Biotechnological Equipment in 2014.Recommanded Product: 27469-60-9 This article mentions the following:

Six new aryl/aralkyl substituted piperazine derivatives, containing methylxanthine moiety I (R = Bn, 4-FC₆H₄, 4-HOC₆H₄, etc.) were synthesized. All compounds were in vitro screened for their activity as antioxidants using DPPH (2,2′-Diphenyl-1-picrylhydrazyl), ABTS (2,2′-azinobis-(3-ethylbenzothiazine-6-sulfonic acid)) and FRAP (ferric reducing/antioxidant power) methods. The antioxidant activity of the studied compounds against lipid peroxidation was also measured. The highest antioxidant activity was demonstrated by compound I (R = 4-HOC₆H₄). It is obvious that the presence of a hydroxyl group in the structure is essential for the antioxidant properties and should be taken into consideration in further design of structures with potential antioxidant properties. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Recommanded Product: 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.Recommanded Product: 27469-60-9

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

Spectrophotometric determination of buclizine and pyrilamine in pharmaceutical formulations by Tpooo was written by Kishore, M.;Hanumantharao, Y.. And the article was included in Analytical Chemistry: An Indian Journal in 2010.Formula: C28H35Cl3N2 This article mentions the following:

A simple, sensitive, selective and accurate spectrophotometric method Tpooo for the determination of buclizine (BUCZ) and pyrilamine (PYRA) in bulk drug and pharmaceutical formulations (tablets) was described. This method is based on the extraction of drugs into organic layer of the dye Tpooo in presence of 0.1 N hydrochloric acid and the absorbances were measured at 480 nm. The results of anal. for this method have been validated statistically and by recovery studies. In the experiment, the researchers used many compounds, for example, 1-(4-(tert-Butyl)benzyl)-4-((4-chlorophenyl)(phenyl)methyl)piperazine dihydrochloride (cas: 129-74-8Formula: C28H35Cl3N2).

1-(4-(tert-Butyl)benzyl)-4-((4-chlorophenyl)(phenyl)methyl)piperazine dihydrochloride (cas: 129-74-8) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Formula: C28H35Cl3N2

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

Synthesis and in Vitro and in Vivo Structure-Activity Relationships of Novel Antifungal Triazoles for Dermatology was written by Meerpoel, Lieven;Backx, Leo J. J.;Van der Veken, Louis J. E.;Heeres, Jan;Corens, David;De Groot, Alex;Odds, Frank C.;Van Gerven, Frans;Woestenborghs, Filip A. A.;Van Breda, Andre;Oris, Michel;Van Dorsselaer, Pascal;Willemsens, Gustaaf H. M.;Vermuyten, Karen J. P.;Marichal, Patrick J. M. G.;Vanden Bossche, Hugo F.;Ausma, Jannie;Borgers, Marcel. And the article was included in Journal of Medicinal Chemistry in 2005.Recommanded Product: 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline This article mentions the following:

In search for new compounds with potential for clin. use as antifungal agents in dermatol., a series of 12 azole compounds, e.g. I, were synthesized stereospecifically and investigated specifically for their activity against dermatophyte fungal infections in animal models. This panel of azoles was studied in vitro and compared with itraconazole and terbinafine for their antifungal activity using a panel of 24 Candida spp. and 182 dermatophyte isolates. Three azoles (I, II, and III) showed in vitro antifungal potency equivalent to itraconazole, but superior to terbinafine, against a panel of 24 Candida spp. With comparable or lower activity than that of itraconazole and terbinafine against 182 dermatophyte isolates and only rare activity against other pathogenic fungi. However, in vivo I and III, both given orally, demonstrated antifungal activity at least three times greater than itraconazole and were superior compared to terbinafine in M. canis infected guinea pigs. In a mouse model infected by T. mentagrophytes, again III, but not I, showed 5-fold superior activity over itraconazole and terbinafine. Compound II was effective in both models but less effective than itraconazole in these models. On the basis of these promising results, III is currently being clin. investigated for its potential as a novel antifungal agent against dermatophytosis. In the experiment, the researchers used many compounds, for example, 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline (cas: 74852-62-3Recommanded Product: 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline).

4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline (cas: 74852-62-3) 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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Recommanded Product: 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline

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

Regulation of cardiac expression of the diabetic marker microRNA miR-29 was written by Arnold, Nicholas;Koppula, Purushotham Reddy;Gul, Rukhsana;Luck, Christian;Pulakat, Lakshmi. And the article was included in PLoS One in 2014.COA of Formula: C19H21F3N6 This article mentions the following:

Diabetes mellitus (DM) is an independent risk factor for heart disease and its underlying mechanisms are unclear. Increased expression of diabetic marker miR-29 family miRNAs (miR-29a, b and c) that suppress the pro-survival protein Myeloid Cell Leukemia 1(MCL-1) is reported in pancreatic β-cells in Type 1 DM. Whether an up-regulation of miR-29 family miRNAs and suppression of MCL-1 (dysregulation of miR-29-MCL-1 axis) occurs in diabetic heart is not known. This study tested the hypothesis that insulin regulates cardiac miR-29-MCL-1 axis and its dysregulation correlates with DM progression. In vitro studies with mouse cardiomyocyte HL-1 cells showed that insulin suppressed the expression of miR-29a, b and c and increased MCL-1 mRNA. Conversely, Rapamycin (Rap), a drug implicated in the new onset DM, increased the expression of miR-29a, b and c and suppressed MCL-1 and this effect was reversed by transfection with miR-29 inhibitors. Rap inhibited mammalian target of rapamycin complex 1 (mTORC1) signaling in HL-1 cells. Moreover, inhibition of either mTORC1 substrate S6K1 by PF-4708671, or eIF4E-induced translation by 4E1RCat suppressed MCL-1. We used Zucker diabetic fatty (ZDF) rat, a rodent model for DM, to test whether dysregulation of cardiac miR-29-MCL-1 axis correlates with DM progression. 11-wk old ZDF rats exhibited significantly increased body weight, plasma glucose, insulin, cholesterol, triglycerides, body fat, heart weight, and decreased lean muscle mass compared to age-matched lean rats. Rap treatment (1.2 mg/kg/day, from 9-wk to 15-wk) significantly reduced plasma insulin, body weight and heart weight, and severely dysregulated cardiac miR-29-MCL1 axis in ZDF rats. Importantly, dysregulation of cardiac miR-29-MCL-1 axis in ZDF rat heart correlated with cardiac structural damage (disorganization or loss of myofibril bundles). We conclude that insulin and mTORC1 regulate cardiac miR-29-MCL-1 axis and its dysregulation caused by reduced insulin and mTORC1 inhibition increases the vulnerability of a diabetic heart to structural damage. In the experiment, the researchers used many compounds, for example, 2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-6-(trifluoromethyl)-1H-benzo[d]imidazole (cas: 1255517-76-0COA of Formula: C19H21F3N6).

2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-6-(trifluoromethyl)-1H-benzo[d]imidazole (cas: 1255517-76-0) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.COA of Formula: C19H21F3N6

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

[The newer antipsychotic cariprazine (reagila): perspectives for use in different stages of schizophrenia therapy]. was written by Ivanov, S V;Voronova, E I. And the article was included in Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova in 2021.Application In Synthesis of 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea This article mentions the following:

Cariprazine is a newer 3rd generation antipsychotic acting as partial agonist for dopamine receptors with unique higher affinity for D3 than D2 receptors. This review article summarizes key data from preclinical and clinical studies of cariprazine including pharmacodynamics, pharmacokinetics, clinical efficacy and safety/acceptability in acute short-term and long-term maintenance and relapse prevention therapy in patients with schizophrenia. Efficacy and safety of cariprazine in patients schizophrenia with predominantly negative symptoms resistant to previous antipsychotic therapy is discussed as well. In the experiment, the researchers used many compounds, for example, 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8Application In Synthesis of 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea).

3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea

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

Discovery, Synthesis, and Bioactivity of Bis(heteroaryl)piperazines. 1. A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors was written by Romero, Donna L.;Morge, Raymond A.;Biles, Carolyn;Berrios-Pena, Norman;May, Paul D.;Palmer, John R.;Johnson, Paul D.;Smith, Herman W.;Busso, Mariano. And the article was included in Journal of Medicinal Chemistry in 1994.Reference of 87394-48-7 This article mentions the following:

A variety of analogs of U-80493E (I) were synthesized and evaluated for their inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). Replacement of the substituted aryl moiety with various substituted indoles provided bis(heteroaryl)piperazines (BHAPs) that were 10-100-fold more potent than U-80493E. The pyridyl portion of the lead mol. was found to be very sensitive to modifications. Extensive preclin. evaluations of several of these compounds led to the selection of U-87201E (atevirdine mesylate) (II) for clin. evaluation. In the experiment, the researchers used many compounds, for example, 1-(3-Nitropyridin-2-yl)piperazine (cas: 87394-48-7Reference of 87394-48-7).

1-(3-Nitropyridin-2-yl)piperazine (cas: 87394-48-7) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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.Reference of 87394-48-7

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