Month: February 2023

Understanding the guest binding in the cucurbit[7]uril inclusion complexes of CDK4/6 inhibitors, palbociclib, and ribociclib from a combined experimental and computational study was written by Katiyar, Dharmendra;Ahamad, Shakir;Dash, Sibananda G.;Tripathi, Sarita;Arora, Ashish;Thakur, Tejender S.. And the article was included in Journal of Molecular Structure in 2021.Reference of 1211441-98-3 This article mentions the following:

We have studied the cucurbit[7]uril inclusion complexes of two anti-cancer drugs, palbociclib and ribociclib, in the solution and solid-state with the help of exptl. and computational approaches. The formation of the cucurbit[7]uril inclusion complex, binding stoichiometry, and binding free energies in aqueous solution was determined from 1H-NMR, UV-spectroscopy and ITC studies. The binding of drugs in the ionized and unionized forms with cucurbit[7]uril was studied with the help of QTAIM anal. and free energy computations. We report the development of new co-amorphous solids of the cucurbit[7]uril inclusion complexes of drugs with enhanced thermal stability. We also report three new crystalline salt forms of palbociclib oxalate and a new DMSO solvate of ribociclib succinate dihydrate in the study. The phase interrelationship between the palbociclib oxalate forms (1a, 1b, and 1c) was established from DSC and PXRD study. In the experiment, the researchers used many compounds, for example, 7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3Reference of 1211441-98-3).

7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3) 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. 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.Reference of 1211441-98-3

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

Synthesis and in vitro antimycobacterial activity of 8-OCH₃ ciprofloxacin methylene and ethylene isatin derivatives was written by Feng, Lian-Shun;Liu, Ming-Liang;Zhang, Shu;Chai, Yun;Wang, Bo;Zhang, Yi-Bin;Lv, Kai;Guan, Yan;Guo, Hui-Yuan;Xiao, Chun-Ling. And the article was included in European Journal of Medicinal Chemistry in 2010.Formula: C18H20FN3O4 This article mentions the following:

A series of novel 8-OCH₃ ciprofloxacin methylene and ethylene isatin derivatives with remarkable improvement in lipophilicity were synthesized in this study. These derivatives were evaluated for their in vitro activity against some mycobacteria. All of the synthesized compounds were less active than the parent 8-OCH₃ ciprofloxacin against Mycobacterium smegmatis CMCC 93202, but most of the methylene isatin derivatives were more active than 8-OCH₃ ciprofloxacin, ciprofloxacin, isoniazid and rifampin against MTB H37Rv ATCC 27294. It was noted that compound I (MIC: 0.074 μM) was 2-13 fold more potent than the reference compounds against MTB H37Rv ATCC 27294, and some compounds (MIC: 6.72-7.05 μM) were around 1.6 fold more potent than the parent 8-OCH₃ ciprofloxacin, 3.5 fold more potent than ciprofloxacin against MDR-MTB 09710. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-6-fluoro-8-methoxy-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 112811-57-1Formula: C18H20FN3O4).

1-Cyclopropyl-6-fluoro-8-methoxy-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 112811-57-1) 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. 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.Formula: C18H20FN3O4

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

Pharmacogenetic variability and the probability of site of action target attainment during tuberculosis meningitis treatment: A physiologically based pharmacokinetic modeling and simulations study was written by Mehta, Krina;Narayanan, Navaneeth;Heysell, Scott K.;Bisson, Gregory P.;Subbian, Selvakumar;Kurepina, Natalia;Kreiswirth, Barry N.;Vinnard, Christopher. And the article was included in Tuberculosis (Oxford, United Kingdom) in 2022.Recommanded Product: 13292-46-1 This article mentions the following:

Our objective was to investigate the role of patient pharmacogenetic variability in determining site of action target attainment during tuberculous meningitis (TBM) treatment. Rifampin and isoniazid PBPK model that included SLCO1B1 and NAT2 effects on exposures resp. were obtained from literature, modified, and validated using available cerebrospinal-fluid (CSF) concentrations Population simulations of isoniazid and rifampin concentrations in brain interstitial fluid and probability of target attainment according to genotypes and M. tuberculosis MIC levels, under standard and intensified dosing, were conducted. The rifampin and isoniazid model predicted steady-state drug concentration within brain interstitial fluid matched with the observed CSF concentrations At MIC level of 0.25 mg/L, 57% and 23% of the patients with wild type and heterozygous SLCO1B1 genotype resp. attained the target in CNS with rifampin standard dosing, improving to 98% and 91% resp. with 35 mg/kg dosing. At MIC level of 0.25 mg/L, 33% of fast acetylators attained the target in CNS with isoniazid standard dosing, improving to 90% with 7.5 mg/kg dosing. In this study, the combined effects of pharmacogenetic and M. tuberculosis MIC variability were potent determinants of target attainment in CNS. The potential for genotype-guided dosing during TBM treatment should be further explored in prospective clin. studies. In the experiment, the researchers used many compounds, for example, 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1Recommanded Product: 13292-46-1).

8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.Recommanded Product: 13292-46-1

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

Efficient matrix cleanup of soft-gel-type dietary supplements for rapid screening of 92 illegal adulterants using EMR-lipid dSPE and UHPLC-Q/TOF-MS was written by Kim, Beom Hee;Lee, Wonwoong;Kim, You Lee;Lee, Ji Hyun;Hong, Jongki. And the article was included in Pharmaceuticals in 2021.Category: piperazines This article mentions the following:

An efficient matrix cleanup method was developed for the rapid screening of 92 illegal adulterants (25 erectile dysfunction drugs, 15 steroids, seven anabolic steroids, 12 antihistamines, 12 nonsteroidal anti-inflammatory drugs (NSAIDs), four diuretics, and 17 weight-loss drugs) in soft-gel-type supplements by ultra-high performance liquid chromatog.-quadrupole/time of flight-mass spectrometry (UHPLC-Q/TOF-MS). As representative green chem. methods, three sample preparation methods (dispersive liquid-liquid microextraction (DLLME), “quick, easy, cheap, effective, rugged, and safe” dispersive solid-phase extraction (QuEChERS-dSPE), and enhanced matrix removal-lipid (EMR-Lipid) dSPE) were evaluated for matrix removal efficiency, recovery rate, and matrix effect. In this study, EMR-Lipid dSPE was shown to effectively remove complicated matrix contents in soft-gels, compared to DLLME and QuEChERS-dSPE. For the rapid screening of a wide range of adulterants, extracted common ion chromatogram (ECIC) and neutral loss scan (NLS) based on specific common MS/MS fragments were applied to randomly collected soft-gel-type dietary supplement samples using UHPLC-Q/TOF-MS. Both ECICs and NLSs enabled rapid and simple screening of multi-class adulterants and could be an alternative to the multiple reaction monitoring (MRM) method. The developed method was validated in terms of limit of detection (LOD), precision, accuracy, recovery, and matrix effects. The range of LODs was 0.1-16 ng/g. The overall precision values were within 0.09-14.65%. The accuracy ranged from 81.6% to 116.6%. The recoveries and matrix effects of 92 illegal adulterants ranged within 16.9-119.4% and 69.8-114.8%, resp. The established method was successfully applied to screen and identify 92 illegal adulterants in soft-gels. This method can be a promising tool for the high-throughput screening of various adulterants in dietary supplements and could be used as a more environmentally friendly routine anal. method for screening dietary supplements illegally adulterated with multi-class drug substances. 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: 224785-90-4Category: piperazines).

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 causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.Category: piperazines

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

Highly Sensitive Built-In Strain Sensors for Polymer Composites: Fluorescence Turn-On Response through Mechanochemical Activation was written by Li, Zhong’an;Toivola, Ryan;Ding, Feizhi;Yang, Jeffrey;Lai, Po-Ni;Howie, Tucker;Georgeson, Gary;Jang, Sei-Hum;Li, Xiaosong;Flinn, Brian D.;Jen, Alex K.-Y.. And the article was included in Advanced Materials (Weinheim, Germany) in 2016.Synthetic Route of C12H16N2O This article mentions the following:

In this paper, the authors report the development of a new class of mechanochromic mols., that can be covalently linked to an epoxy thermoset network as built-in fluorescent strain sensors through simple and facile chem. Under mech. deformation, the sensing mols. in the epoxy matrix undergo a force-induced elimination reaction to regenerate the conjugated pathway between the donor and the acceptor forming a dipolar structure with strong intramol. charge-transfer. This sensor system can be activated even at a very low deformation strain about 0.14 accompanied with a fluorescence “turn-on” response, and is stable under prolonged exposure to light, demonstrating the significant value for practical applications of strain/damage sensing. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1Synthetic Route of C12H16N2O).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) 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. 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).Synthetic Route of C12H16N2O

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

Synthesis and anti-tumor activity evaluation of a novel series of dithiocarbamates bearing 1,2,3-triazole and [1-Bi(4-fluorophenyl)methyl]piperazine unit was written by Mo, Song;Ding, Yong;Zhang, Gang;Zhang, Zhen;Shao, Xuebei;Li, Qinghan;Yang, Xuejun;Chen, Feng. And the article was included in Youji Huaxue in 2017.Formula: C17H18F2N2 This article mentions the following:

Sixteen novel dithiocarbamates containing 1,2,3-triazole and [1-bi(4-fluorophenyl)methyl]piperazine group were prepared via two steps starting from [1-bis(4-fluorophenyl)methyl]piperazine, propargyl bromide, methanedithione and sodium azide, using a very simple catalytic system composed of 5 mol% copper(I) iodide and MDF-H₂O (V:V = 1:1) as solvent at 70°C for 4 h with moderate yield (34%-65%). The structures of the new compounds were characterized by IR, MS, ¹H NMR, ¹³C NMR and element anal. The bioactive assay for the newly prepared compounds manifested that fourteen dithiocarbamate derivatives exhibited good to excellent inhibitory activity against CDC25B in 20μg/mL (inhibitory rate up to 97.96%, IC₅₀ value up to 11.55μg/mL), and six dithiocarbamate derivatives exhibited excellent inhibitory activity against leukemia HL-60 and lung cancer A-549 cell in 40μmol·L^-1 (inhibitory rate up to 99.99% and 93.91%, resp.; IC₅₀ value up to 12.11 and 22.45μg/mL, resp.). In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Formula: C17H18F2N2).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) 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 formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Formula: C17H18F2N2

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

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).

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

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

Incidence, characteristics and risk factors for drug-induced liver injury in hospitalized patients: A matched case-control study was written by Kong, Xianghao;Guo, Daihong;Liu, Siyuan;Zhu, Yu;Yu, Chengxuan. And the article was included in British Journal of Clinical Pharmacology in 2021.Quality Control of (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid This article mentions the following:

The diagnosis of drug-induced liver injury (DILI) is relatively complex and involves a wide variety of drugs. The purpose of this study was to use algorithms to quickly screen DILI patients, determine its incidence and identify risk factors. The Adverse Drug Events Active Surveillance and Assessment System-2 was used to extract the data of patients hospitalized in 2019 according to the set standards and the Roussel Uclaf Causality Assessment Method was used to evaluate patients who met the standards A retrospective case-control study was conducted according to suspected drugs, length of hospital stay and height- and weight-matched controls, and logistic regression was used to identify risk factors. Among the 156 570 hospitalized patients, 480 patients (499 cases) with DILI were confirmed and the incidence of DILI was 0.32%. Anti-infective agents, antineoplastic agents and nonsteroidal anti-inflammatory drugs were the major categories of drugs causing DILI, and the highest incidence of DILI was due to voriconazole. The latency period and hospital stay of patients with cholestasis were both relatively long. Patients with hyperlipidemia (adjusted odds ratio [AOR] 1.884), cardiovascular disease (AOR 1.465), pre-existing liver disease (AOR 1.827) and surgical history (AOR 1.312) were at higher risk for DILI. The incidence of DILI in hospitalized patients was uncommon (0.32%) and its pathogenic drugs were widely distributed. The incidence of DILI for many drugs has been seriously underestimated. It is recommended to focus on patients with hyperlipidemia, cardiovascular disease, pre-existing liver disease and surgical history. In the experiment, the researchers used many compounds, for example, (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0Quality Control of (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid).

(6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.Quality Control of (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

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

Phosphodiesterase type-5 inhibitors for erectile dysfunction following nerve-sparing radical prostatectomy: A network meta-analysis was written by Yang, Jie;Jian, Zhong-Yu;Wang, Jia. And the article was included in Medicine (Philadelphia, PA, United States) in 2021.Recommanded Product: 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one This article mentions the following:

To verify which phosphodiesterase type 5 inhibitors (PDE5is) strategy is better for erectile dysfunction (ED) following nerve-sparing radical prostatectomy (NSRP). This systematic literature search was conducted in MEDLINE, Web of Science and Cochrane Central Register of Controlled Trials database to identify eligible studies from the startup of these databases to 1 Nov., 2019. The ED recovery rate was the main outcome. Traditional pair-wise meta-anal. and multivariate random-effects network meta-anal. (NMA) were performed to explore direct and indirect comparisons, resp. The surface under the cumulative ranking (SUCRA) probabilities was used to evaluate the efficacy of treatments. A total of 14 randomized controlled trials with four kinds of PDE5is were included. Further pooled evidence suggested that PDE5is followed by NSRP had a benefit for penile rehabilitation compared to placebo using traditional pair-wise meta-analyses. Our NMA showed that Avanafil 200mg on demand might be most likely to be the best treatment option according to the first rank of SUCRA both in NMA (SUCRA 83.5) and sensitivity anal. (SUCRA 90.2). Avanafil 200mg on demand has the highest probability of being the best intervention among PDE5is in treating ED following NSRP. However, more randomized controlled trials are needed to validate this in consideration of the published data regarding Avanafil is relatively small scale. 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: 224785-90-4Recommanded Product: 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one).

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 belongs to the family of medicines called anthelmintics. 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.Recommanded Product: 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one

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

Tandospirone reduces wasting and improves cardiac function in experimental cancer cachexia. was written by Elkina, Yulia;Palus, Sandra;Tschirner, Anika;Hartmann, Kai;von Haehling, Stephan;Doehner, Wolfram;Mayer, Ulrike;Coats, Andrew J S;Beadle, John;Anker, Stefan D;Springer, Jochen. And the article was included in International journal of cardiology in 2013.HPLC of Formula: 112457-95-1 This article mentions the following:

BACKGROUND: Cancer cachexia is thought to be the cause of >20% of cancer related deaths. Symptoms of cancer cachexia patients include depression and anorexia significantly worsening their quality of life. Moreover, in rodent models of cancer cachexia atrophy of the heart has been shown to impair cardiac function. Here, we characterize the effects of the antidepressant and anxiolytic drug tandospirone on wasting, cardiac function and survival in experimental cancer cachexia. METHODS: The well-established Yoshida hepatoma rat model was used and tumor-bearing rats were treated with 1mg/kg/d (LD), 10mg/kg/d (HD) tandospirone or placebo. Weight, body composition (NMR), cardiac function (echocardiography), activity and food intake were assessed. Noradrenalin and cortisol were measured in plasma and caspase activity in skeletal muscle. RESULTS: Ten mg/kg/d tandospirone decreased the loss of body weight (p=0.0003) compared to placebo animals, mainly due to preservation of muscle mass (p<0.001), while 1mg/kg/d tandospirone was not effective. Locomotor activity (p=0.0007) and food intake (p=0.0001) were increased by HD tandospirone. The weight (p=0.0277) and function of heart (left ventricular mass, fractional shortening, stroke volume, ejection fraction, all p<0.05) were significantly improved. In the HD tandospirone group, plasma levels of noradrenalin and cortisol were significantly reduced by 49% and 52%, respectively, which may have contributed to the lower caspase activity in the gastrocnemius muscle. Most importantly, HD tandospirone significantly improved survival compared to placebo rats (HR: 0.34; 95% CI: 0.13-0.86; p=0.0495). CONCLUSION: Tandospirone showed significant beneficial effects in the Yoshida hepatoma cancer cachexia model and should be further examined as a prospective drug for this syndrome. In the experiment, the researchers used many compounds, for example, rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1HPLC of Formula: 112457-95-1).

rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1) 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. 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: 112457-95-1

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