Heterocyclic Building Blocks-piperidine

TCTP protein degradation by targeting mTORC1 and signaling through S6K, Akt, and Plk1 sensitizes lung cancer cells to DNA-damaging drugs was written by Jeong, Mini;Jeong, Mi Hyeon;Kim, Jung Eun;Cho, Serin;Lee, Kyoung Jin;Park, Serkin;Sohn, Jeongwon;Park, Yun Gyu. And the article was included in Scientific Reports in 2021.SDS of cas: 1255517-76-0 This article mentions the following:

Translationally controlled tumor protein (TCTP) is expressed in many tissues, particularly in human tumors. It plays a role in malignant transformation, apoptosis prevention, and DNA damage repair. The signaling mechanisms underlying TCTP regulation in cancer are only partially understood. Here, we investigated the role of mTORC1 in regulating TCTP protein levels, thereby modulating chemosensitivity, in human lung cancer cells and an A549 lung cancer xenograft model. The inhibition of mTORC1, but not mTORC2, induced ubiquitin/proteasome-dependent TCTP degradation without a decrease in the mRNA level. PLK1 activity was required for TCTP ubiquitination and degradation and for its phosphorylation at Ser⁴⁶ upon mTORC1 inhibition. Akt phosphorylation and activation was indispensable for rapamycin-induced TCTP degradation and PLK1 activation, and depended on S6K inhibition, but not mTORC2 activation. Furthermore, the minimal dose of rapamycin required to induce TCTP proteolysis enhanced the efficacy of DNA-damaging drugs, such as cisplatin and doxorubicin, through the induction of apoptotic cell death in vitro and in vivo. This synergistic cytotoxicity of these drugs was induced irresp. of the functional status of p53. These results demonstrate a new mechanism of TCTP regulation in which the mTORC1/S6K pathway inhibits a novel Akt/PLK1 signaling axis and thereby induces TCTP protein stabilization and confers resistance to DNA-damaging agents. The results of this study suggest a new therapeutic strategy for enhancing chemosensitivity in lung cancers regardless of the functional status of p53. 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: 1255517-76-0SDS of cas: 1255517-76-0).

2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-6-(trifluoromethyl)-1H-benzo[d]imidazole (cas: 1255517-76-0) 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. 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.SDS of cas: 1255517-76-0

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

Automated determination of phenothiazine drugs by spectrophotometry with palladium(II) chloride was written by Sawada, Minoru;Motoyama, Ichiro;Yamada, Sachiko;Kanaya, Yoshikiyo. And the article was included in Bunseki Kagaku in 1986.COA of Formula: C22H30N4O2S2 This article mentions the following:

An automated assay for phenothiazine drugs using a PdCl₂ solution was established by application of a continuous flow anal. A sample was dissolved in a mixture of 0.625M H₂SO₄ and DMF (2:3) to make about 3 × 10^-3M solution A standard solution was prepared in the same way. A 4.2 × 10^-3M PdCl₂ stock solution was prepared by dissolving PdCl₂ in 0.625M H₂S₄ and diluted with DMF (4:1) before use. Using an automatic analyzer, the sample solution was diluted with a mixture of 0.625M H₂SO₄ and DMF (4:1) to one-seventh of the concentration, and the diluted sample solution was added to a 6-fold volume of the PdCl₂ solution The absorbance of this mixture was determined at 490 nm. The accuracy was 99-100% except pharmaceutical preparations containing excess chloride and the reproducibility was 0.1-0.3%. It was possible to assay up to 30 samples per day which are 2- to 3-fold more than those handled manually. The continuous variation methods showed that the Pd complex was a 1:1 of Pd-phenothiazine. The absorption at about 490 nm resulting from the Pd complex was affected by substituents at 2- and 10-positions of a phenothiazine 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: 316-81-4COA of Formula: C22H30N4O2S2).

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. 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: C22H30N4O2S2

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

Dummy molecularly imprinted solid phase extraction in a nylon membrane filter for analysis of vardenafil in health care products was written by Wan, Libin;Gao, Huoliang;Gao, Haidong;Yan, Ge;Wang, Fayun;Wang, Yong;Chen, Mantang. And the article was included in Microchemical Journal in 2021.Recommanded Product: 224785-90-4 This article mentions the following:

A novel dummy molecularly imprinted polymer (MIP) was prepared for highly specific recognition of vardenafil. Sildenafil was used as the template, and Fe-based metal-organic gel was in situ formed and acted as structural modulator and porogenic agent. The obtained MIP was demonstrated to have stronger binding affinity and higher binding capacity towards vardenafil than non-imprinted polymer (NIP). Adsorption processes of vardenafil on MIP and NIP were fitted well by Freundlich isotherm model. Combined with LC-MS anal. a miniaturized solid phase extraction (SPE) method using MIP as the adsorbent and using a syringe connected with a nylon membrane filter as the adsorbent container was developed. Under the optimal extraction parameters, trace vardenafil has been extraction by the developed method from the spiked water sample with satisfied recovery of 104%, and the intra- and inter-day relative standard deviations (RSDs) were below 7.3%. The linear range was 10-1000 ng mL^-1 (R² = 0.9996), and the limit of detection (LOD, S/N = 3) and limit of quantification (LOQ, S/N = 10) were 1.8 and 6.0μg L^-1, resp. Finally, the proposed MIP-SPE-LC/MS method was applied to discover vardenafil from health care products (HCPs) using standard addition method. The repeatability for both HCPs was below 6.3% (RSD values). Anal. results implied that the developed MIP-SPE-LC/MS method is green, convenient and useful to monitor the illegal additives in HCPs. 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: 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. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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. Recommanded Product: 224785-90-4

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

Towards a defined ECM and small molecule based monolayer culture system for the expansion of mouse and human intestinal stem cells was written by Tong, Zhixiang;Martyn, Keir;Yang, Andy;Yin, Xiaolei;Mead, Benjamin E.;Joshi, Nitin;Sherman, Nicholas E.;Langer, Robert S.;Karp, Jeffrey M.. And the article was included in Biomaterials in 2018.Quality Control of 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline This article mentions the following:

Current ISC culture systems face significant challenges such as animal-derived or undefined matrix compositions, batch-to-batch variability (e.g. Matrigel-based organoid culture), and complexity of assaying cell aggregates such as organoids which renders the research and clin. translation of ISCs challenging. Here, through screening for suitable ECM components, we report a defined, collagen based monolayer culture system that supports the growth of mouse and human intestinal epithelial cells (IECs) enriched for an Lgr5⁺ population comparable or higher to the levels found in a standard Matrigel-based organoid culture. The system, referred to as the Bolstering Lgr5 Transformational (BLT) Sandwich culture, comprises a collagen IV-coated porous substrate and a collagen I gel overlay which sandwich an IEC monolayer in between. The distinct collagen cues synergistically regulate IEC attachment, proliferation, and Lgr5 expression through maximizing the engagement of distinct cell surface adhesion receptors (i.e. integrin α2β1, integrin β4) and cell polarity. Further, we apply our BLT Sandwich system to identify that the addition of a bone morphogenetic protein (BMP) receptor inhibitor (LDN-193189) improves the expansion of Lgr5-GFP⁺ cells from mouse small intestinal crypts by nearly 2.5-fold. Notably, the BLT Sandwich culture is capable of expanding human-derived IECs with higher LGR5 mRNA levels than conventional Matrigel culture, providing superior expansion of human LGR5⁺ ISCs. Considering the key roles Lgr5⁺ ISCs play in intestinal epithelial homeostasis and regeneration, we envision that our BLT Sandwich culture system holds great potential for understanding and manipulating ISC biol. in vitro (e.g. for modeling ISC-mediated gut diseases) or for expanding a large number of ISCs for clin. utility (e.g. for stem cell therapy). In the experiment, the researchers used many compounds, for example, 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1062368-24-4Quality Control of 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline).

4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1062368-24-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.Quality Control of 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

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

Identification and quantification of the antipsychotics risperidone, aripiprazole, pipamperone and their major metabolites in plasma using ultra-high performance liquid chromatography-mass spectrometry was written by Wijma, Rixt A.;van der Nagel, Bart C. H.;Dierckx, Bram;Dieleman, Gwen C.;Touw, Daan J.;van Gelder, Teun;Koch, Birgit C. P.. And the article was included in Biomedical Chromatography in 2016.Safety of 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one This article mentions the following:

The antipsychotics risperidone, aripiprazole and pipamperone are frequently prescribed for the treatment in children with autism. The aim of this study was to validate an ultra-high performance liquid chromatog.-mass spectrometry method for the quantification of these antipsychotics in plasma. An ultra-high performance liquid chromatog.-mass spectrometry assay was developed for the determination of the drugs and metabolites. Gradient elution was performed on a reversed-phase column with a mobile phase consisting of ammonium acetate, formic acid in methanol or in Milli-Q ultrapure water at a flow rate of 0.5 mL/min. The method was validated according to the US Food and Drug Administration guidelines. The analytes were found to be stable enough after reconstitution and injection of only 5 μL improved the accuracy and precision in combination with the internal standard Calibration curves of all five analytes were linear. All analytes were stable for at least 72 h in the autosampler and the high quality control of 9-OH-risperidone was stable for 48 h. The method allows quantification of all analytes. The advantage of this method is the combination of a minimal injection volume, a short run-time, an easy sample preparation method and the ability to quantify all analytes in one run. Copyright © 2015 John Wiley & Sons, Ltd. In the experiment, the researchers used many compounds, for example, 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 129722-25-4Safety of 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one).

7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 129722-25-4) 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.Safety of 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one

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

Klebsiella pneumoniae invasion syndrome: a case of liver abscess combined with lung abscess, endophthalmitis, and brain abscess was written by Zhang, Chen-Guang;Wang, Yan;Duan, Min;Zhang, Xiang-Yang;Chen, Xu-Yan. And the article was included in Journal of International Medical Research in 2022.Recommanded Product: 62893-19-0 This article mentions the following:

Klebsiella pneumoniae invasion syndrome (KPIS) is a critical multi-site infection that is usually caused by highly virulent Klebsiella pneumonia. It is relatively common in Asian patients with diabetes and leads to sepsis, which has a high mortality rate. We report the case of a man in his early 40s who presented to the hospital with blurred vision in his left eye of 7 days’ duration and fever of 1 day’s duration. After a complete examination, he was diagnosed with KPIS on the basis of his liver abscessation, lung abscessation, endophthalmitis of the left eye and brain abscessation. After needle puncture and drainage of the left eye and liver abscess and anti-bacterial treatment with meropenem, the patient recovered well. When KPIS is suspected, attention should be paid to the sites of infection and the selection of the most appropriate antibiotics, but the most important aim should be to drain the lesions in a timely manner to improve the patient’s prognosis. 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: 62893-19-0Recommanded Product: 62893-19-0).

(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 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. Recommanded Product: 62893-19-0

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

Inhibition of angiogenesis by the antifungal drug itraconazole was written by Chong, Curtis R.;Xu, Jing;Lu, Jun;Bhat, Shridhar;Sullivan, David J. Jr.;Liu, Jun O.. And the article was included in ACS Chemical Biology in 2007.Quality Control of 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline This article mentions the following:

Angiogenesis, the formation of new blood vessels, is implicated in a number of important human diseases, including cancer, diabetic retinopathy, and rheumatoid arthritis. To identify clin. useful angiogenesis inhibitors, the authors assembled and screened a library of mostly Food and Drug Administration-approved drugs for inhibitors of human endothelial cell proliferation. One of the most promising and unexpected this was itraconazole, a known antifungal drug. Itraconazole inhibits endothelial cell cycle progression at the G1 phase in vitro and blocks vascular endothelial growth factor/basic fibroblast growth factor-dependent angiogenesis in vivo. In attempts to delineate the mechanism of action of itraconazole the authors found that human lanosterol 14α-demethylase (14DM) is essential for endothelial cell proliferation and may partially mediate the inhibition of endothelial cells by itraconazole. Together, these findings suggest that itraconazole has the potential to serve as an antiangiogenic drug and that lanosterol 14DM is a promising new target for discovering new angiogenesis inhibitors. In the experiment, the researchers used many compounds, for example, 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline (cas: 74852-62-3Quality Control of 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline).

4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline (cas: 74852-62-3) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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. Quality Control of 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline

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

Copulatory Dyskinesia: Pathognomonic Manifestation of Tardive Dyskinesia. was written by Sharma, Vibhash D;Gupta, Harsh V;Espay, Alberto J. And the article was included in Tremor and other hyperkinetic movements (New York, N.Y.) in 2020.Synthetic Route of C25H27N3O2S This article mentions the following:

Background: Copulatory or pelvic thrusting dyskinesia is a subtype of tardive dyskinesia (TD) which is caused by exposure to dopamine blocking agents. Phenomenology shown: A man exhibiting rhythmic, stereotypical pelvic thrusting movements. Educational value: Recognition of copulatory dyskinesia as a distinctive iatrogenic disorder helps prevent unnecessary investigations and guides the implementation of corrective strategies. In the experiment, the researchers used many compounds, for example, 7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 913611-97-9Synthetic Route of C25H27N3O2S).

7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 913611-97-9) 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.Synthetic Route of C25H27N3O2S

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

Inhibition of bone morphogenetic protein 6 receptors ameliorates Sjogren’s syndrome in mice was written by Yin, Hongen;Kalra, Lovika;Lai, Zhennan;Guimaro, Maria C.;Aber, Lauren;Warner, Blake M.;Michael, Drew;Zhang, Nan;Cabrera-Perez, Javier;Karim, Arif;Swaim, William D.;Afione, Sandra;Voigt, Alexandria;Nguyen, Cuong Q.;Yu, Paul B.;Bloch, Donald B.;Chiorini, John A.. And the article was included in Scientific Reports in 2020.Synthetic Route of C25H22N6 This article mentions the following:

Primary Sjogren’s syndrome (pSS) is a chronic autoimmune disease, with only palliative treatments available. Recent work has suggested that increased bone morphogenetic protein 6 (BMP6) expression could alter cell signaling in the salivary gland (SG) and result in the associated salivary hypofunction. We examined the prevalence of elevated BMP6 expression in a large cohort of pSS patients and tested the therapeutic efficacy of BMP signaling inhibitors in two pSS animal models. Increased BMP6 expression was found in the SGs of 54% of pSS patients, and this increased expression was correlated with low unstimulated whole saliva flow rate. In mouse models of SS, inhibition of BMP6 signaling reduced phosphorylation of SMAD1/5/8 in the mouse submandibular glands, and led to a recovery of SG function and a decrease in inflammatory markers in the mice. The recovery of SG function after inhibition of BMP6 signaling suggests cellular plasticity within the salivary gland and a possibility for therapeutic intervention that can reverse the loss of function in pSS. In the experiment, the researchers used many compounds, for example, 5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1432597-26-6Synthetic Route of C25H22N6).

5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1432597-26-6) 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. 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. Synthetic Route of C25H22N6

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

Improvement and validation of rapid simultaneous analysis method for veterinary drugs by LC-MS/MS (part 2) was written by Fujii, Yoshiaki;Kaga, Takero;Hosokawa, Aoi;Nishimura, Kazuhiko. And the article was included in Hokkaidoritsu Eisei Kenkyushoho in 2019.Application of 113617-63-3 This article mentions the following:

Veterinary drugs (animal drugs) are drugs used for the treatment and prevention of diseases of livestock and households, and play an important role in the stable supply of livestock products. This paper discusses improvement and validation of rapid simultaneous anal. method for veterinary drugs by liquid chromatog.-mass spectrometry/mass spectrometry. The substances and medicines to be examined, the sources of standard products and LC-MS/MS conditions were given. The calibration curve was prepared using the matrix standard solution, and validity evaluation test was carried out. In this anal. method, every methods were simplified and good results were obtained compare to previous report. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3Application of 113617-63-3).

1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3) 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.Application of 113617-63-3

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