Month: February 2023

Nalfurafine hydrochloride enabled to reduce dosage or discontinue conventional treatment for uremic pruritus was written by Yoshizawa, Taku;Kumagai, Junko;Takahashi, Naoko;Tsuchiya, Shinichiro. And the article was included in Jin to Toseki in 2013.Application In Synthesis of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride This article mentions the following:

In this paper, nalfurafine hydrochloride enabled to reduce dosage or discontinue conventional treatment for uremic pruritus was reported. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3Application In Synthesis of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride).

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3) 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.Application In Synthesis of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride

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

Reduction of bitterness of antihistaminic drugs by complexation with β-cyclodextrins was written by Ono, Nao;Miyamoto, Yuji;Ishiguro, Takako;Motoyama, Keiichi;Hirayama, Fumitoshi;Iohara, Daisuke;Seo, Hakaru;Tsuruta, Satoshi;Arima, Hidetoshi;Uekama, Kaneto. And the article was included in Journal of Pharmaceutical Sciences in 2011.Synthetic Route of C21H29Cl3N2O2 This article mentions the following:

Reduction of bitterness of antihistaminic drugs by cyclodextrin (CyD) complexation was examined The stability constant (Kc) of the 1:1 CyD inclusion complexes with antihistaminic drugs increased in the order of 2-hydroxypropyl-β-CyD (HP-β-CyD) ≈ β-CyD > γ-CyD > α-CyD for diphenhydramine and epinastine, and HP-β-CyD ≈ β-CyD > α-CyD > γ-CyD for hydroxyzine, cetirizine, and dl-chlorpheniramine. The inclusion complexes inhibited the adsorption of antihistaminic drugs to lipid membrane using liposomes, as the magnitude of Kc increased. From human gustatory sensation tests, β-CyD and HP-β-CyD potently suppressed the bitterness of antihistaminic drugs in a dose-dependent manner. Further, an artificial taste sensor anal. revealed that β-CyD and HP-β-CyD inhibited the bitterness of antihistaminic drugs in solution The results suggest that CyDs suppress the bitterness of antihistaminic drugs in solutions through the formation of inclusion complexes. These results may provide useful information for masking or elimination of bitterness of drugs using CyDs. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:1935-1943, 2011. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3Synthetic Route of C21H29Cl3N2O2).

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3) 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.Synthetic Route of C21H29Cl3N2O2

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

Synthesis, biological evaluation and structure-activity correlation study of a series of imidazol-based compounds as Candida albicans inhibitors was written by Moraca, Francesca;De Vita, Daniela;Pandolfi, Fabiana;Di Santo, Roberto;Costi, Roberta;Cirilli, Roberto;D’Auria, Felicia Diodata;Panella, Simona;Palamara, Anna Teresa;Simonetti, Giovanna;Botta, Maurizio;Scipione, Luigi. And the article was included in European Journal of Medicinal Chemistry in 2014.Recommanded Product: 87394-48-7 This article mentions the following:

A new series of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives was synthesized. The antifungal activity was evaluated in vitro against different fungal species. The biol. results show that the most active compounds possess an antifungal activity comparable or higher than Fluconazole against Candida albicans, non-albicans Candida species, Cryptococcus neoformans and dermathophytes. Because of their racemic nature, the most active compounds I and II were tested as pure enantiomers. For II the (R)-enantiomer resulted more active than the (S)-one, otherwise for 5f the (S)-enantiomer resulted the most active. To rationalize the exptl. data, a ligand-based computational study was carried out; the results of the modeling study show that (S)-I and (R)-II perfectly align to the ligand-based model, showing the same relative configuration. Preliminary studies on the human lung adenocarcinoma epithelial cells (A549) have shown that II, III and I possess a low cytotoxicity. In the experiment, the researchers used many compounds, for example, 1-(3-Nitropyridin-2-yl)piperazine (cas: 87394-48-7Recommanded Product: 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 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: 87394-48-7

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

miR-217-5p regulates myogenesis in skeletal muscle stem cells by targeting FGFR2 was written by Zhu, Menghai;Chen, Gang;Yang, Yi;Yang, Jiantao;Qin, Bengang;Gu, Liqiang. And the article was included in Molecular Medicine Reports in 2020.Quality Control of rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide This article mentions the following:

MicroRNA-217-5p (miR-217-5p) has been implicated in cell proliferation; however, its role in skeletal muscle stem cells (SkMSCs) remains unknown. The present study aimed to explore the roles of miR-217-5p in the biol. characteristics of SkMSCs. SkMSCs were identified by cell surface markers using flow cytometry. The present study observed that miR-217-5p mimics accelerated the proliferation and suppressed the differentiation in SkMSCs. In addition, the results of the present study revealed that fibroblast growth factor receptor 2 (FGFR2) was a target of miR-217-5p, as miR-217-5p bound directly to the 3′-untranslated region of FGFR2 mRNA, resulting in increased FGFR2 mRNA and protein levels. In addition, the present study suppressed the expression of FGFR2 in SkMSCs using a selective FGFR inhibitor AZD4547 and detected the efficiency of inhibition by reverse transcription-quant. PCR and western blotting. miR-217-5p levels were pos. associated with FGFR2 expression, which was upregulated and accelerated the proliferation of SkMSCs compared with that of the miR-NC group. MiR-217-5p levels were pos. associated with FGFR2 expression, which was upregulated and accelerated the proliferation of SkMSCs compared with that of the miR-NC group. Collectively, these results demonstrated that miR-217-5p may act as a myogenesis promoter in SkMSCs by directly targeting FGFR2 and may regulate the myogenesis of these cells. 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: 1035270-39-3Quality Control of rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide).

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. 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 rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide

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

Synthesis of new hexahydropyrimido[1,2-a]azepine derivatives bearing functionalized aryl and heterocyclic moieties as anti-inflammatory agents was written by Hassanein, Hassanein H.;Abdel Rahman, Doaa E.;Fouad, Marwa A.;Ahmed, Rehab F.. And the article was included in Future Medicinal Chemistry in 2021.HPLC of Formula: 27913-99-1 This article mentions the following:

New hexahydropyrimido[1,2-a]azepine derivatives bearing functionalized aryl and heterocyclic moieties were synthesized as anti-inflammatory agents with better safety profiles. All synthesized compounds were assessed in vitro for their COX-1 and COX-2 inhibition activities. The most selective compounds, 2f, 5 and 6, were further evaluated for their in vivo anti-inflammatory activity and PGE2 inhibitory activity. To rationalize their selectivity, mol. docking within COX-1 and COX-2 binding sites was performed. Their physicochem. properties and drug-like nature profile were also calculated The good activity and selectivity of compounds 2f, 5 and 6 were rationalized using a mol. docking study and supported by in vivo studies. These promising findings are encouraging for performing future investigations of these derivatives In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1HPLC of Formula: 27913-99-1).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) 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.HPLC of Formula: 27913-99-1

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

Application of a 2D-QSAR with a sine normalization method for the biodegradation of fluoroquinolones to poison cyanobacteria was written by Li, Minghao;Du, Meijin;Sun, Ruihao;Zhang, Wenhui;Hou, Yilin;Li, Yu. And the article was included in Environmental Science and Pollution Research in 2021.Recommanded Product: 113617-63-3 This article mentions the following:

Abstract: Cyanobacteria are photosynthetic autotrophic aquatic prokaryotes. One of the methods for controlling cyanobacterial blooms is to destroy the phycobiliproteins required for photosynthesis. In this study, to improve the biodegradation of the fluoroquinolones through inhibit cyanobacteria, the mol. docking scores of 32 fluoroquinolones (FQs) with four categories of phycobiliproteins from cyanobacteria were calculated after sine normalization to characterize the binding ability between them. A two-dimensional quant. structure-activity relationship (2D-QSAR) model was constructed based on the comprehensive scores. Danofloxacin (DAN) with the highest comprehensive score was chosen for mol. modification. When docking with four categories of phycobiliproteins from cyanobacteria, the docking values of DAN-11 and DAN-16 were increased up to 35.75%. Moreover, their functional characteristics and environmentally friendly predictive values were improved. When the DAN-11 and DAN-16 mols. docked with the other cyanobacterial phycobiliproteins, indicating that the designed DAN derivatives had general applicability to poison cyanobacteria, the weak interaction forces might increase the binding ability between the DAN derivatives and the receptor phycobiliprotein compared with the target mol. 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: 113617-63-3Recommanded Product: 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. Simple N-substituted piperazines have been found in many drug molecules. 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: 113617-63-3

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

TB-PRACTECAL: study protocol for a randomised, controlled, open-label, phase II-III trial to evaluate the safety and efficacy of regimens containing bedaquiline and pretomanid for the treatment of adult patients with pulmonary multidrug-resistant tuberculosis was written by Berry, Catherine;du Cros, Philipp;Fielding, Katherine;Gajewski, Suzanne;Kazounis, Emil;McHugh, Timothy D.;Merle, Corinne;Motta, Ilaria;Moore, David A. J.;Nyang’wa, Bern-Thomas. And the article was included in Trials in 2022.Synthetic Route of C43H58N4O12 This article mentions the following:

Globally rifampicin-resistant tuberculosis disease affects around 460,000 people each year. Currently recommended regimens are 9-24 mo duration, have poor efficacy and carry significant toxicity. A shorter, less toxic and more efficacious regimen would improve outcomes for people with rifampicin-resistant tuberculosis. TB-PRACTECAL is an open-label, randomised, controlled, phase II/III non-inferiority trial evaluating the safety and efficacy of 24-wk regimens containing bedaquiline and pretomanid to treat rifampicin-resistant tuberculosis. Conducted in Uzbekistan, South Africa and Belarus, patients aged 15 and above with rifampicin-resistant pulmonary tuberculosis and requiring a new course of therapy were eligible for inclusion irresp. of HIV status. In the first stage, equivalent to a phase IIB trial, patients were randomly assigned one of four regimens, stratified by site. Investigational regimens include oral bedaquiline, pretomanid and linezolid. Addnl., two of the regimens also included moxifloxacin (arm 1) and clofazimine (arm 2) resp. Treatment was administered under direct observation for 24 wk in investigational arms and 36 to 96 wk in the standard of care arm. The second stage of the study was equivalent to a phase III trial, investigating the safety and efficacy of the most promising regimen/s. The primary outcome was the percentage of unfavorable outcomes at 72 wk post-randomisation. This was a composite of early treatment discontinuation, treatment failure, recurrence, lost-to-follow-up and death. The study is being conducted in accordance with ICH-GCP and full ethical approval was obtained from Medecins sans Frontieres ethical review board, London School of Hygiene and Tropical Medicine ethical review board as well as ERBs and regulatory authorities at each site. TB-PRACTECAL is an ambitious trial using adaptive design to accelerate regimen assessment and bring novel treatments that are effective and safe to patients quicker. The trial took a patient-centered approach, adapting to best practice guidelines throughout recruitment. The implementation faced significant challenges from the COVID-19 pandemic. The trial was terminated early for efficacy on the advice of the DSMB and will report on data collected up to the end of recruitment and, addnl., the planned final anal. at 72 wk after the end of recruitment. Trial registration: Clinicaltrials.gov NCT02589782. Registered on 28 Oct. 2015. In the experiment, the researchers used many compounds, for example, 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1Synthetic Route of C43H58N4O12).

8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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 C43H58N4O12

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

Analysis of the correlation of structure and properties of antihistamine drugs was written by Kirillova, O. V.;Belyaeva, A. S.;Kolchina, G. U.;Zharennikova, N. V.;Safiullina, I. I.;Lopatinskaya, N. E.;Movsumzade, E. M.. And the article was included in Bashkirskii Khimicheskii Zhurnal in 2017.Computed Properties of C28H35Cl3N2 This article mentions the following:

The study deals with chem. drugs which have anti-allergic properties and is used in the last decade in our country and abroad. Anti-allergic properties dependence on the structure of certain classes of chem. compounds is demonstrated. An attempt assessing the impact of the individual units and groupings of atoms on the properties of the study drug is presented. AU the pharmacolo-gical properties of different classes of antihista-mines are displayed in table. In the experiment, the researchers used many compounds, for example, 1-(4-(tert-Butyl)benzyl)-4-((4-chlorophenyl)(phenyl)methyl)piperazine dihydrochloride (cas: 129-74-8Computed Properties of C28H35Cl3N2).

1-(4-(tert-Butyl)benzyl)-4-((4-chlorophenyl)(phenyl)methyl)piperazine dihydrochloride (cas: 129-74-8) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Computed Properties of C28H35Cl3N2

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

Pharmacological activity of compounds isolated from methanolic extract marine sponge xestospongia sp. against escherichia coli and staphylococcus aureus was written by Fristiohady, A.;Wahyuni;Sadarun, B.;Bafadal, M.;Andriani, R.;Purnama, L. O. M. J.;Malik, F.;Ilyas, M.;Malaka, M. H.;Sahidin, I.. And the article was included in Journal of Physics: Conference Series in 2021.Application In Synthesis of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol This article mentions the following:

Few previous studies show pharmacol. potencies of Xestospongia sp. and have not been explored further about its antibacterial activity. Thus, this study aims to isolate and identify the isolates from Xestospongia sp. and testing their antibacterial activity. Xestospongia Sp. was macerated with methanol then isolated and was purified by using vacuum liquid chromatog. (VLC), radial chromatog. (RC) and thin-layer chromatog. (TLC). Isolated compounds then analyzed, identified, and determined their structures using 1H-NMR Spectrophotometer and by comparising data to references and ChemDraw 8.0. Compounds obtained with various concentrations (1000; 500; 100μg/mL) then tested against Staphylococcus aureus ATCC 25923 and Escherichia coli ATCC 35218 using agar welldiffuse method. According to the study, two compounds isolated which were Saringosterol (isolate X1) and predicted-compound halenaquinone (isolate X2). The antibacterial test showed that isolate X1 was unable to inhibit bacteria’s’ growth at each concentration, and isolate X2 showed antibacterial activity against S. aureus ATCC 25923 and E. coli ATCC 35218 at concentration 1000 and 500μg/mL. In conclusion, 2 compounds successfully isolated from methanolic extract of Xestospongia sp. which were Saringosterol and predicted-compound halenaquninone, and only predicted-compound halenaquinone showed antibacterial activity at concentration 1000 and 500μg/mL. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol (cas: 68-88-2Application In Synthesis of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol).

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. 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.Application In Synthesis of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol

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

Inhibition of FGFR2 enhances chemosensitivity to gemcitabine in cholangiocarcinoma through the AKT/mTOR and EMT signaling pathways was written by Jaidee, Rattanaporn;Kukongviriyapan, Veerapol;Senggunprai, Laddawan;Prawan, Auemduan;Jusakul, Apinya;Laphanuwat, Phatthamon;Kongpetch, Sarinya. And the article was included in Life Sciences in 2022.HPLC of Formula: 872511-34-7 This article mentions the following:

To investigate the oncogenic role of FGFR2 in carcinogenesis in cholangiocarcinoma (CCA) cells. In addition, the feasibility of using FGFR inhibitors in combination with standard chemotherapy was also explored for the chemosensitizing effect in CCA cells. Five CCA cell lines were used to screen FGFR2 expression by Western immunoblotting. Two CCA cell lines, KKU-100 and KKU-213A, were knocked down of the FGFR2 gene using siRNA. Cell viability was assessed by the MTS cell proliferation assay. Reproductive cell death was assessed by clonogenic assay. The effects on cell migration and invasion were analyzed by the Transwell chamber method. Cell cycle anal. was performed by flow cytometry. Cell angiogenesis was assessed by HUVEC tube formation and human angiogenesis antibody array anal. Proteins associated with proliferative and metastatic properties were evaluated by Western blotting. Knockdown of FGFR2 suppressed cell growth and colony formation in CCA cells in association with G2/M cell cycle arrest and downregulation of STAT3, cyclin A and cyclin B1. Silencing FGFR2 enhanced the suppressive effect of gemcitabine (Gem) on cell migration and invasion. The combination of infigratinib, an FGFR inhibitor, and Gem, interrupted cell growth, migration, and invasion via downregulation of FGFR/AKT/mTOR pathways and the EMT-associated proteins vimentin and slug. Moreover, the combination also suppressed tube formation together with decreased expression of the proangiogenic factor VEGF. Inhibition of FGFRs by infigratinib enhanced the antitumor effect of Gem in CCA cells through downregulation of the FGFR/AKT/mTOR, FGFR/STAT3 and EMT signaling pathways. In the experiment, the researchers used many compounds, for example, 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7HPLC of Formula: 872511-34-7).

3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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: 872511-34-7

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