Category: piperazines

Novel Organic Salts Based on Mefloquine: Synthesis, Solubility, Permeability, and In Vitro Activity against Mycobacterium tuberculosis was written by Silva, Dario;Lopes, Marcio V. C.;Petrovski, Zeljko;Santos, Miguel M.;Santos, Jussevania P.;Yamada-Ogatta, Sueli F.;Bispo, Marcelle L. F.;de Souza, Marcus V. N.;Duarte, Ana Rita C.;Lourenco, Maria C. S.;Goncalves, Raoni Schroeder B.;Branco, Luis C.. And the article was included in Molecules in 2022.Product Details of 75277-39-3 This article mentions the following:

The development of novel pharmaceutical tools to efficiently tackle tuberculosis is the order of the day due to the rapid development of resistant strains of Mycobacterium tuberculosis. Herein, we report novel potential formulations of a repurposed drug, the antimalarial mefloquine (MFL), which was combined with organic anions as chem. adjuvants. Eight mefloquine organic salts were obtained by ion metathesis reaction between mefloquine hydrochloride ([MFLH][Cl]) and several organic acid sodium salts in high yields. One of the salts, mefloquine mesylate ([MFLH][MsO]), presented increased water solubility in comparison with [MFLH][Cl]. Moreover, all salts with the exception of mefloquine docusate ([MFLH][AOT]) showed improved permeability and diffusion through synthetic membranes. Finally, in vitro activity studies against Mycobacterium tuberculosis revealed that these ionic formulations exhibited up to 1.5-times lower MIC values when compared with [MFLH][Cl], particularly mefloquine camphorsulfonates ([MFLH][(1R)-CSA], [MFLH][(1S)-CSA]) and mefloquine HEPES ([MFLH][HEPES]). In the experiment, the researchers used many compounds, for example, Sodium 2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate (cas: 75277-39-3Product Details of 75277-39-3).

Sodium 2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate (cas: 75277-39-3) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 75277-39-3

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

Low-dose vardenafil potentiates the protective effect of (-)-epigallocatechin gallate on cardiomyocytes was written by Wang, Kai;Fan, Zhaoyang;Jin, Peng;Qin, Dingkui;Du, Qizhen. And the article was included in Pakistan Journal of Pharmaceutical Sciences in 2020.Synthetic Route of C23H32N6O4S This article mentions the following:

The major polyphenol (-)-epigallocatechin gallate (EGCG) of green tea shows well-known health benefits such as potential anti-cancer, anti-oxidation and ameliorating cardiovascular disease. This work aims to improve the bioactivity of EGCG on H9C2 cardiomyocytes by combination regimen of vardenafil and EGCG. The proliferative rates were significantly improved by 18.74%, 10.77% and 29.17% after 48 h with EGCG, vardenafil, and the combination of EGCG and low-dose vardenafil treatments, resp. The treatments also increased the expression of the nitric oxide synthase (eNOS), and acutely stimulate production of vasodilators nitric oxide (NO) from 17.33micromol/L to 19.75, 20.87 and 24.47μmol/L in H9C2 cells. We further demonstrated that vardenafil also remarkably promoted EGCG to counteract H2O2-induced apoptotic damage in H9C2 by strengthening antioxidant defense systems and suppressing myocardial apoptosis. These results suggest that EGCG and low-dose vardenafil in combination may be a promising regimen to help prevent cardiovascular diseases. 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: 224785-90-4Synthetic Route 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. 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.Synthetic Route of C23H32N6O4S

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

Solid-Phase-Fluorimetric Determination of Quinolones in Medicinal Preparations on Cellulose Paper and in a Thin Silica Layer Using a Smartphone was written by Amelin, V. G.;Shogah, Z. A. Ch.;Bol′shakov, D. S.. And the article was included in Journal of Analytical Chemistry in 2021.Related Products of 98105-99-8 This article mentions the following:

A simple and an available method is proposed for the determination of quinolone antibiotics using solid-phase fluorescence digital colorimetry. The intrinsic fluorescence of 17 quinolones and the quinolone-sensitizedfluorescence of europium on cellulose paper (CP) and a thin silica layer are studied. Upon the irradiation of quinolone solutions applied to a matrix with UV light (365 nm), blue (CP, high-performance thin-layer chromatog. (HPTLC)) and pink (CP-Eu, HPTLC-Eu) fluorescence is observed Measurement of the fluorescence intensity on the surface of matrixes is carried out using a smartphone. The values of colorimetric parameters in the RGB system are used as the anal. signal (A_r): A_r = (R₀-R_x)² + (G₀-G_x)² (B₀-B_x)² The limits of detection and determination are 0.2-4 and 0.6-12 μg/mL, resp., for all analyzed analytes. The anal. ranges are 0.6-500 μg/mL. A procedure for the determination of fluoroquinolones in medicinal preparations is proposed. The relative standard deviation of the results of anal. does not exceed 5%. In the experiment, the researchers used many compounds, for example, 6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 98105-99-8Related Products of 98105-99-8).

6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 98105-99-8) 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. Related Products of 98105-99-8

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

Preclinical Pharmacological Evaluation of a Novel Multiple Kinase Inhibitor, ON123300, in Brain Tumor Models was written by Zhang, Xiaoping;Lv, Hua;Zhou, Qingyu;Elkholi, Rana;Chipuk, Jerry E.;Reddy, M. V. Ramana;Reddy, E. Premkumar;Gallo, James M.. And the article was included in Molecular Cancer Therapeutics in 2014.COA of Formula: C24H27N7O This article mentions the following:

ON123300 is a low mol. weight multikinase inhibitor identified through a series of screens that supported further analyses for brain tumor chemotherapy. Biochem. assays indicated that ON123300 was a strong inhibitor of Ark5 and CDK4, as well as growth factor receptor tyrosine kinases such as β-type platelet-derived growth factor receptor (PDGFRβ). ON123300 inhibited U87 glioma cell proliferation with an IC₅₀ 3.4 ± 0.1 μmol/L and reduced phosphorylation of Akt, yet it also unexpectedly induced Erk activation, both in a dose- and time-dependent manner that subsequently was attributed to relieving Akt-mediated C-Raf S259 inactivation and activating a p70S6K-initiated PI3K-neg. feedback loop. Cotreatment with the EGFR inhibitor gefitinib produced synergistic cytotoxic effects. Pursuant to the in vitro studies, in vivo pharmacokinetic and pharmacodynamic studies of ON123300 were completed in mice bearing intracerebral U87 tumors following i.v. doses of 5 and 25 mg/kg alone, and also at the higher dose concurrently with gefitinib. ON123300 showed high brain and brain tumor accumulation based on brain partition coefficient values of at least 2.5. Consistent with the in vitro studies, single agent ON123300 caused a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors, whereas addition of gefitinib to the ON123300 regimen significantly enhanced p-Akt inhibition and prevented Erk activation. In summary, ON123300 demonstrated favorable pharmacokinetic characteristics, and future development for brain tumor therapy would require use of combinations, such as gefitinib, that mitigate its Erk activation and enhance its activity. Mol Cancer Ther; 13(5); 1105-16. ©2014 AACR. In the experiment, the researchers used many compounds, for example, 8-Cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile (cas: 1357470-29-1COA of Formula: C24H27N7O).

8-Cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile (cas: 1357470-29-1) 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. 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.COA of Formula: C24H27N7O

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

Antibiotics in elderly Chinese population and their relations with hypertension and pulse pressure was written by Li, Zhenkun;Liu, Kaiyong;Zhao, Jianing;Yang, Linsheng;Chen, Guimei;Liu, Annuo;Wang, Qunan;Wang, Sufang;Li, Xiude;Cao, Hongjuan;Tao, Fangbiao;Zhang, Dongmei. And the article was included in Environmental Science and Pollution Research in 2022.HPLC of Formula: 98105-99-8 This article mentions the following:

Although antibiotic exposure in the general population has been well documented by a biomonitoring approach, epidemiol. data on the relationships between urinary antibiotic burden in the elderly with blood pressure (BP) are still lacking. The current study revealed thirty-four antibiotics in urine specimens from 990 elderly patients in Lu’an City, China, with detection frequencies ranging from 0.2 to 35.5%. Among the elderly, the prevalence of hypertension was 72.0%, and 12 antibiotics were detected in more than 10% of individuals with hypertension. The elderly with hypertension had the maximum daily exposure (5450.45μg/kg/day) to fluoroquinolones (FQs). Multiple linear regression analyses revealed significant associations of BP and pulse pressure (PP) with exposure to specific antibiotics. The estimated β values (95% confidence interval) of associations with systolic blood pressure (SBP) in the right arm were 4.42 (1.15, 7.69) for FQs, 4.26 (0.52, 8.01) for the preferred as human antibiotics (PHAs), and 3.48 (0.20, 6.77) for the mixtures (FQs + tetracyclines [TCs] (tertile 3 vs. tertile 1)), resp. Increased concentrations of TCs were associated with decreased diastolic BP (DBP; tertile 3: -1.75 [-3.39, -0.12]) for the right arm. Higher levels of FQs (tertile 3: 4.28 [1.02, 7.54]), PHAs (tertile 3: 4.25 [0.49, 8.01]), and FQs + TCs (tertile 3: 3.99 [0.71, 7.26]) were associated with increased SBP, and an increase in DBP for FQs (tertile 3: 1.82 [0.22, 3.42]) was shown in the left arm. Also, higher urinary concentrations of FQs (tertile 3: 3.18 [0.53, 5.82]), PHAs (tertile 3: 3.42 [0.40, 6.45]), and FQs + TCs (tertile 3: 3.06 [0.40, 5.72]) were related to increased PP, whereas a decline in PP for TCs (tertile 2: -2.93 [-5.60, -0.25]) in the right arm. And increased concentrations of penicillin V (tertile 3: 5.31 [1.53, 9.10]) and FQs + TCs (tertile 3: 2.84 [0.19, 5.49]) were related to higher PP in the left arm. By utilizing restricted cubic splines, our current study revealed a potential nonlinear dose-response association between FQ exposure and hypertension risk. In conclusion, this investigation is the first to present antibiotic exposure using a biomonitoring approach, and informs understanding of impacts of antibiotic residues, as emerging hazardous pollutants, on the hypertension risk in the elderly. In the experiment, the researchers used many compounds, for example, 6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 98105-99-8HPLC of Formula: 98105-99-8).

6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 98105-99-8) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.HPLC of Formula: 98105-99-8

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

The application of the MM/GBSA method in the binding pose prediction of FGFR inhibitors was written by Chen, Yu;Zheng, Yongxiang;Fong, Pedro;Mao, Shengjun;Wang, Qiantao. And the article was included in Physical Chemistry Chemical Physics in 2020.COA of Formula: C26H33N5O3 This article mentions the following:

The success of a structure-based drug is highly dependent on a known binding pose of the protein-ligand system. However, this is not always available. The authors set out to explore the applicability of the popular and easy-to-use MD-based MM/GBSA method to determine the binding poses of known FGFR inhibitors. MM/GBSA combined with 100 ns of MD simulation significantly improved the success rate of docking methods from 30-40% to 70%. This work demonstrates a way that the MM/GBSA method can be more accurate than it is in ligand ranking, filling a gap in structure-based drug discovery when the binding pose is unknown. In the experiment, the researchers used many compounds, for example, rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3COA of Formula: C26H33N5O3).

rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.COA of Formula: C26H33N5O3

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

Binding kinetics of cariprazine and aripiprazole at the dopamine D₃ receptor was written by Frank, Annika;Kiss, Dora J.;Keseru, Gyoergy M.;Stark, Holger. And the article was included in Scientific Reports in 2018.Computed Properties of C21H32Cl2N4O This article mentions the following:

The dissociation behaviors of aripiprazole and cariprazine at the human D₂ and D₃ receptor are evaluated. A potential correlation between kinetics and in vivo profiles, especially cariprazine’s action on neg. symptoms in schizophrenia, is investigated. The binding kinetics of four ligands were indirectly evaluated. After the receptor preparations were pre-incubated with the unlabeled ligands, the dissociation was initiated with an excess of [³H]spiperone. Slow dissociation kinetics characterizes aripiprazole and cariprazine at the D₂ receptor. At the D₃ receptor, aripiprazole exhibits a slow monophasic dissociation, while cariprazine displays a rapid biphasic behavior. Functional ss-arrestin assays and mol. dynamics simulations at the D₃ receptor confirm a biphasic binding behavior of cariprazine. This may influence its in vivo action, as the partial agonist could react rapidly to variations in the dopamine levels of schizophrenic patients and the ligand will not quant. dissociate from the receptor in one single step. With these findings novel agents may be developed that display rapid, biphasic dissociation from the D₃R to further investigate this effect on in vivo profiles. 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: 839712-12-8Computed Properties of C21H32Cl2N4O).

3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.Computed Properties of C21H32Cl2N4O

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

Evidence of N-acetylcysteine efficacy for skin picking disorder: A retrospective cohort study was written by Hwang, Angelina S.;Campbell, Elliott H.;Sartori-Valinotti, Julio C.. And the article was included in Journal of the American Academy of Dermatology in 2022.SDS of cas: 68-88-2 This article mentions the following:

Skin picking disorder (SPD) is defined as a repetitive skin manipulation, resulting in visible tissue damage and the impairment of social functioning. There have not been consistent pos. responses to previous treatment options, 2 evidence supports the use of N-acetylcysteine (NAC) for SPD. The highest level of evidence comes from a randomized control trial (RCT) with psychiatric endpoints evaluated by psychiatrists. This was a single-center, retrospective study, subjects were identified using the following search terms from medical records on 2 sep. encounters: (acetylcysteine) AND ([picking] OR [acne excoriee] OR [neurodermatitis]). A patient was deemed to have a pos. treatment response if there was an objective improvement documented in the phys. examination and assessment sections of the clin. note. Of 28 participants meeting the inclusion criteria, 85.7% were women, the pos. response rate was 61.5% among 13 patients with an adequate trial (min. dosage of 600 mg twice daily for 3 consecutive months or equivalent dose). The overall response rate (including in those without an adequate trial) was 46.4%. The side effects included gastrointestinal symptoms in 7.1% of the patients, the average age of patients with SPD improvement was 68.5 years vs. 50.9 years of those without improvement. The purpose of our study was to corroborate the results of a previous RCT performed by psychiatrists using predominantly psychiatric end points. Our study focused on dermatol. endpoints observed by dermatologists. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol (cas: 68-88-2SDS of cas: 68-88-2).

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol (cas: 68-88-2) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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. SDS of cas: 68-88-2

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

March 1964 and corrections was written by Anonymous. And the article was included in Federal Register in 1964.Recommanded Product: 142-64-3 This article mentions the following:

The following new drugs have been approved for human use: ethynylestradiol and norethindrone acetate; aspirin, phenacetin, caffeine and orphenadrine citrate; norethindrone and mestranol; lidocaine, Bi subgallate, ZnO, Al subacetate, and Peruvian balsam; nalidixic acid; lidocaine; pralidoxime chloride; ammonium form of cross-linked polyacrylic (carboxylic) cation-exchange resin; and for veterinary use: trichlorfon, phenothiazine, and piperazine-di-HCl. In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3Recommanded Product: 142-64-3).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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).Recommanded Product: 142-64-3

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

Efficacy of FGFR inhibitors and combination therapies for acquired resistance in FGFR2-fusion cholangiocarcinoma was written by Krook, Melanie A.;Lenyo, Alexandria;Wilberding, Max;Barker, Hannah;Dantuono, Mikayla;Bailey, Kelly M.;Chen, Hui-Zi;Reeser, Julie W.;Wing, Michele R.;Miya, Jharna;Samorodnitsky, Eric;Smith, Amy M.;Dao, Thuy;Martin, Dorrelyn M.;Ciombor, Kristen K.;Hays, John;Freud, Aharon G.;Roychowdhury, Sameek. And the article was included in Molecular Cancer Therapeutics in 2020.Related Products of 1035270-39-3 This article mentions the following:

Thus, there is a critical need for the development of innovative therapeutic strategies to overcome acquired drug resistance. Here, we present findings from a patient with FGFR2-altered metastatic cholangiocarcinoma who enrolled in a phase II clin. trial of the FGFR inhibitor, infigratinib (BGJ398). Treatment was initially effective as demonstrated by imaging and tumor marker response; however, after eight months on trial, the patient exhibited tumor regrowth and disease progression. Targeted sequencing of tumor DNA after disease progression revealed the FGFR2 kinase domain p.E565A and p.L617M single nucleotide variants (SNVs) hypothesized to drive acquired resistance to infigratinib. The sensitivities of these FGFR2 SNVs, which were detected post-infigratinib therapy, were extended to include clin. relevant FGFR inhibitors including AZD4547, erdafitinib (JNJ-42756493), dovitinib, ponatinib, and TAS120, and were evaluated in vitro. Through a proteomics approach, we identified upregulation of the PI3K/AKT/mTOR signaling pathway in cells harboring the FGFR2 p.E565A mutation and demonstrated that combination therapy strategies with FGFR and mTOR inhibitors may be used to overcome resistance to FGFR inhibition, specific to infigratinib. Collectively, these studies support the development of novel combination therapeutic strategies in addition to the next generation of FGFR inhibitors to overcome acquired resistance in patients. In the experiment, the researchers used many compounds, for example, rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3Related Products of 1035270-39-3).

rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Related Products of 1035270-39-3

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