Month: February 2023

Identification of the Clinical Development Candidate MRTX849, a Covalent KRAS^G12C Inhibitor for the Treatment of Cancer was written by Fell, Jay B.;Fischer, John P.;Baer, Brian R.;Blake, James F.;Bouhana, Karyn;Briere, David M.;Brown, Karin D.;Burgess, Laurence E.;Burns, Aaron C.;Burkard, Michael R.;Chiang, Harrah;Chicarelli, Mark J.;Cook, Adam W.;Gaudino, John J.;Hallin, Jill;Hanson, Lauren;Hartley, Dylan P.;Hicken, Erik J.;Hingorani, Gary P.;Hinklin, Ronald J.;Mejia, Macedonio J.;Olson, Peter;Otten, Jennifer N.;Rhodes, Susan P.;Rodriguez, Martha E.;Savechenkov, Pavel;Smith, Darin J.;Sudhakar, Niranjan;Sullivan, Francis X.;Tang, Tony P.;Vigers, Guy P.;Wollenberg, Lance;Christensen, James G.;Marx, Matthew A.. And the article was included in Journal of Medicinal Chemistry in 2020.Synthetic Route of C11H19N3O2 This article mentions the following:

Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new technologies and strategies are aiding in the target’s resurgence. As previously reported, the tetrahydropyridopyrimidines were identified as irreversible covalent inhibitors of KRAS^G12C that bind in the switch-II pocket of KRAS and make a covalent bond to cysteine 12. Using structure-based drug design in conjunction with a focused in vitro absorption, distribution, metabolism and excretion screening approach, analogs were synthesized to increase the potency and reduce metabolic liabilities of this series. The discovery of the clin. development candidate MRTX849(I)as a potent, selective covalent inhibitor of KRAS^G12C is described. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl 3-(cyanomethyl)piperazine-1-carboxylate (cas: 1589082-06-3Synthetic Route of C11H19N3O2).

(S)-tert-Butyl 3-(cyanomethyl)piperazine-1-carboxylate (cas: 1589082-06-3) 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.Synthetic Route of C11H19N3O2

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

Anti-infective composite cryogel scaffold treats osteomyelitis and augments bone healing in rat femoral condyle was written by Qayoom, Irfan;Srivastava, Ekta;Kumar, Ashok. And the article was included in Biomaterials Advances in 2022.COA of Formula: C43H58N4O12 This article mentions the following:

Bone and joint infections pose a serious challenge in the orthopedic medical condition which presents a major health care problem and economic burden to the patients. The current treatment strategies adopted have a very limited successful outcome in majority of the cases and need serious reconsiderations in terms of management, diagnosis and effective treatment approach. Herein, we have developed a composite cryogel scaffold from nanohydroxyapatite and collagen mimicking natural bone composition for the local delivery of antibiotic to treat osteomyelitis. The biomimetic and biodegradable antibiotic-loaded composite scaffold was found to be biocompatible with potent osteogenic capacity and anti-infective characteristics under in vitro conditions. Moreover, the anti-infective potency of the antibiotic-loaded composite cryogel was also evaluated in rat osteomyelitis model to cure the infection and promote bone healing. It was observed that anti-infective collagen-nanohydroxyapatite composite cryogel when loaded with bone morphogenetic protein-2 (BMP-2) and zoledronic acid (ZA) could completely eradicate the infection in rat femoral condyle and simultaneously, accelerate bone healing at the dead space created during surgical procedures. The approach developed in this study is the development of biomimetic and bioactive composite carrier of antibiotics for the treatment of bone infection. The findings of this study insinuate that this antibiotic-loaded composite cryogel scaffold could potentially be used as an anti-infective biomaterial for the treatment of bone infections which will simultaneosuly promote bone healing at the dead space created during surgical procedures. In the experiment, the researchers used many compounds, for example, 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1COA of Formula: C43H58N4O12).

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. 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).COA of Formula: C43H58N4O12

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

Treatment shortening of drug-sensitive pulmonary tuberculosis using high-dose rifampicin for 3 months after culture conversion (Hi-DoRi-3): a study protocol for an open-label randomized clinical trial was written by Kwak, Nakwon;Jeon, Doosoo;Park, Youngmok;Kang, Young Ae;Kim, Kyung Jong;Kim, Young Ran;Kwon, Byoung Soo;Kwon, Yong-Soo;Kim, Hyung-Jun;Lee, Jae Ho;Lee, Ji Yeon;Lee, Jung-Kyu;Mok, Jeongha;Cheon, Minkyoung;Park, Jiwon;Hahn, Seokyung;Yim, Jae-Joon. And the article was included in Trials in 2022.SDS of cas: 13292-46-1 This article mentions the following:

The standard treatment regimen for drug-sensitive tuberculosis (TB), comprising four companion drugs, requires a min. duration of 6 mo, and this lengthy treatment leads to poor adherence and increased toxicity. To improve rates of adherence, reduce adverse events, and lower costs, a simplified and shortened treatment regimen is warranted. This study is a multicenter, open-label randomized clin. trial of non-inferiority design that compares a new regimen with the conventional regimen for drug-sensitive pulmonary TB. The investigational group will use a regimen of high-dose rifampicin (30 mg/kg/day) with isoniazid and pyrazinamide, and the treatment will be maintained for 12 wk after the achievement of neg. conversion of sputum culture. The control group will be treated for 6 mo with a World Health Organization-endorsed regimen consisting of isoniazid, rifampicin (10 mg/kg/day), ethambutol, and pyrazinamide. The primary endpoint is the proportion of unfavorable outcomes at 18 mo after randomization. Secondary outcomes include time to unfavorable treatment outcome, time to culture conversion on liquid medium, treatment success rate at the end of treatment, proportion of recurrence at 18 mo after randomization, time to recurrence after treatment completion, and adverse events of grade 3 or higher during the treatment. We predict a 10% unfavorable outcome for the control group, and 0% difference from the investigational group. Based on 80% verification power and a 2.5% one-sided significance level for a non-inferiority margin of 6%, 393 participants per group are required. Considering the 15% dropout rate, a total of 926 participants (463 in each group) will be recruited. This study will inform on the feasibility of the treatment regimen using high-dose rifampicin with a shortened and individualized treatment duration for pulmonary TB. Trial registration: ClinicalTrials.gov NCT04485156. In the experiment, the researchers used many compounds, for example, 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1SDS of cas: 13292-46-1).

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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.SDS of cas: 13292-46-1

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

Role of Fibroblast Growth Factors in the Crosstalk of Hepatic Stellate Cells and Uveal Melanoma Cells in the Liver Metastatic Niche was written by Seitz, Tatjana;John, Nora;Sommer, Judith;Dietrich, Peter;Thasler, Wolfgang E.;Hartmann, Arndt;Evert, Katja;Lang, Sven A.;Bosserhoff, Anja;Hellerbrand, Claus. And the article was included in International Journal of Molecular Sciences in 2022.Synthetic Route of C26H31Cl2N7O3 This article mentions the following:

Hepatic metastasis is the critical factor determining tumor-associated mortality in different types of cancer. This is particularly true for uveal melanoma (UM), which almost exclusively metastasizes to the liver. Hepatic stellate cells (HSCs) are the precursors of tumor-associated fibroblasts and support the growth of metastases. However, the underlying mechanisms are widely unknown. Fibroblast growth factor (FGF) signaling is dysregulated in many types of cancer. The aim of this study was to analyze the pro-tumorigenic effects of HSCs on UM cells and the role of FGFs in this crosstalk. Conditioned medium (CM) from activated human HSCs significantly induced proliferation together with enhanced ERK and JNK activation in UM cells. An in silico database anal. revealed that there are almost no mutations of FGF receptors (FGFR) in UM. However, a high FGFR expression was found to be associated with poor survival for UM patients. In vitro, the pro-tumorigenic effects of HSC-CM on UM cells were abrogated by a pharmacol. inhibitor (BGJ398) of FGFR1/2/3. The expression anal. revealed that the majority of paracrine FGFs are expressed by HSCs, but not by UM cells, including FGF9. Furthermore, the immunofluorescence anal. indicated HSCs as a cellular source of FGF9 in hepatic metastases of UM patients. Treatment with recombinant FGF9 significantly enhanced the proliferation of UM cells, and this effect was efficiently blocked by the FGFR1/2/3 inhibitor BGJ398. Our study indicates that FGF9 released by HSCs promotes the tumorigenicity of UM cells, and thus suggests FGF9 as a promising therapeutic target in hepatic metastasis. 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: 872511-34-7Synthetic Route of C26H31Cl2N7O3).

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. 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.Synthetic Route of C26H31Cl2N7O3

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

A pooled post hoc analysis evaluating the safety and tolerability of cariprazine in bipolar depression was written by Earley, Willie R.;Burgess, Maria;Rekeda, Ludmyla;Hankinson, Arlene;McIntyre, Roger S.;Suppes, Trisha;Calabrese, Joseph R.;Yatham, Lakshmi N.. And the article was included in Journal of Affective Disorders in 2020.Electric Literature of C21H32Cl2N4O This article mentions the following:

The safety and efficacy of cariprazine, a dopamine D3-preferring D3/D2 receptor partial agonist and serotonin 5-HT1A receptor partial agonist, was evaluated in 4 randomized, double-blind, placebo-controlled trials in patients with bipolar depression. Safety and tolerability were evaluated in 2 post hoc analyses. Modal dose anal.: pooled data from all 4 flexible/fixed-dose trials (dose groups: <1.5, 1.5, 3 mg/d). Fixed-dose anal.: pooled data from 2 identically designed fixed-dose trials (1.5 and 3 mg/d dose groups). The modal dose and fixed-dose analyses evaluated data from 1775 and 970 patients, resp. Cariprazine was generally safe and well tolerated; study completion rates were 78% and 82% in the modal dose and fixed-dose analyses, resp. In modal dose anal., treatment-emergent adverse events (TEAEs) occurred in 60% of overall cariprazine- and 55% of placebo-treated patients; nausea (8% vs 3%) and akathisia (7% vs 2%) occurred in ≥5% of cariprazine patients and twice the rate of placebo. Metabolic changes were small and generally similar for cariprazine and placebo; mean increase in glucose was 3.1 mg/dL for cariprazine and 2.6 mg/dL for placebo. Fixed-dose and modal dose findings were generally consistent; values for most metabolic parameters were slightly higher for fixed-dose 3 mg/d vs. 1.5 mg/d. Post hoc analyses, modal dose groups, short treatment duration. In modal dose (0.25-3 mg/d) and fixed-dose (1.5 and 3 mg/d) analyses, cariprazine was generally safe and well tolerated in the treatment of bipolar depression. Slightly improved tolerability was observed with fixed-dose cariprazine 1.5 mg/d vs. 3 mg/d. 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: 839712-12-8Electric Literature 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 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.Electric Literature of C21H32Cl2N4O

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

A Precise Molecular Design to Achieve ACQ-to-AIE Transformation for Developing New Mechanochromic Material by Regio-Isomerization Strategy was written by Liu, Wei;Wang, Xinli;Li, Renfu;Sun, Shitao;Li, Zhenli;Hao, Jinle;Lin, Bin;Jiang, Hong;Xie, Lijun. And the article was included in ChemistrySelect in 2022.Application of 27913-99-1 This article mentions the following:

Herein, we have designed and synthesized a series of MeO-rofecoxib based fluorophore (MORF1-6) for exploiting new promising mechanochromic luminescent (MCL) materials. Among them, MORF1 and MORF3 exhibit aggregation-induced emission (AIE) effects when the substituent is located at the ortho-position on the benzene ring of b. Meanwhile, by changing the type and position of the substituent, the corresponding compounds MORF2, MORF4, MORF5, MORF6 show aggregation caused-quenching (ACQ) behavior. These results demonstrate that the position and type of the substituent have a great effect on their fluorescent properties. Furthermore, an X-ray crystal structure anal. of MORF3 revealed that the intermol. π-π stacking was suppressed and intramol. hydrogen bonding were formed, which could effectively restrict the mol. motions, thus causing typical AIE effect and mechanochromic property. Finally, a re-writable data recording device was fabricated using MORF3 as the active material. Our mol. design strategy may provide a new avenue for achieving efficient MCL materials. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1Application of 27913-99-1).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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 of 27913-99-1

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

Characterization and identification of SFDC -1, a novel AmpC -type β-lactamase in Serratia fonticola was written by Dong, Xu;Zhang, Peiyao;Zhou, Kexin;Liang, Jialei;Li, Qiaoling;Zhang, Xueya;Zhou, Danying;Lu, Wei;Sun, Zhewei;Liu, Hongmao;Lu, Junwan;Lin, Xi;Li, Kewei;Xu, Teng;Zhang, Hailin;Zhu, Mei;Bao, Qiyu. And the article was included in Environmental Microbiology in 2021.Recommanded Product: (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 clin. and environmental infections caused by AmpC β-lactamases have been increasingly reported recently. In this study, we characterize the novel chromosome-encoded AmpC β-lactamase SFDC-1 identified in Serratia fonticola strain R28, which was isolated from a rabbit raised on a farm in southern China. SFDC-1 shared the highest amino acid identity of 79.6% with the functionally characterized AmpC β-lactamase gene blaYRC-1, although it had highly homologous functionally uncharacterized relatives in the same species from different sources, including some of the clin. significance. The cloned blaSFDC-1 exhibited resistance to a broad spectrum of β-lactam antibiotics, including most cephalosporins with the highest resistance to ampicillin, cefazolin and ceftazidime, with increased MIC levels ≥128-fold compared with the control strains. The purified SFDC-1 showed catalytic activities against β-lactams with the highest catalytic activity to cefazolin. The genetic context of blaSFDC-1 and its relatives was conserved in the chromosome, and no mobile genetic elements were found surrounding them. The nucleotide sequences of the chromosome and two plasmids (pR28_180 and pR28_75) of Serratia fonticola R28 and the blaSFDC-1 gene in this work have been submitted to the GenBank database under accession numbers CP072742, CP072743, CP072744 and MW896115 resp. 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: (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. Simple N-substituted piperazines have been found in many drug molecules. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Recommanded Product: (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

The kinase inhibitor TKI258 is active against the novel CUX1-FGFR1 fusion detected in a patient with T-lymphoblastic leukemia/lymphoma and t(7;8)(q22;p11) was written by Wasag, Bartosz;Lierman, Els;Meeus, Peter;Cools, Jan;Vandenberghe, Peter. And the article was included in Haematologica in 2011.HPLC of Formula: 692737-80-7 This article mentions the following:

We report a patient with T-lymphoblastic leukemia/lymphoma and a t(7;8)(q22;p11). CUX1 was identified as the fusion partner of FGFR1 by fluorescence in situ hybridization and 5′ RACE-PCR. We further investigated this novel FGFR1 fusion using the interleukin-3 (IL-3) dependent Ba/F3 cell line and demonstrated IL-3 independent cell growth of CUX1-FGFR1 expressing cells. TKI258 and PKC412 potently inhibited proliferation of CUX1-FGFR1 transformed Ba/F3 cells. This growth inhibition was shown to be mediated by inhibition of CUX1-FGFR1 kinase activity for TKI258 but not PKC412. In summary, we identified a novel CUX1-FGFR1 fusion oncogene in a patient with the 8p11 myeloproliferative syndrome and demonstrated its transforming potential in the Ba/F3 cell line. Our in vitro data support the further investigation of TKI258 for the treatment of constitutively active FGFR1 fusion proteins. In the experiment, the researchers used many compounds, for example, 4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate (cas: 692737-80-7HPLC of Formula: 692737-80-7).

4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate (cas: 692737-80-7) 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: 692737-80-7

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

Formulation and evaluation of orodispersible film of hydroxyzine hydrochloride was written by Jani, Rupal;Patel, Reeni;Shah, Pratik. And the article was included in World Journal of Pharmaceutical Research in 2015.Quality Control of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride This article mentions the following:

In the present study, an attempt was made to develop orodispersible film of Hydroxyzine Hydrochloride by solvent casting method. Drugexcipients and excipients-excipients incompatibility study was carried out using fourier transform IR Spectroscopy (FTIR) which shows that drug-excipient and excipient-excipient were compatible to each other. Orodispersible film of Hydroxyzine Hydrochloride containing hydroxy Pr Me cellulose E5LV and hydroxy Pr Me cellulose E15LV were developed by solvent casting method using propylene glycol as a plasticizer and citric acid as a saliva stimulating agent. Batch H1 (hydroxy Pr Me cellulose E15LV 100 mg, citric acid 20 mg and propylene glycol 20% weight/weight) showed excellent appearance, transparency,% elongation 1.7 ± 0.30,tensile strength 35 ± 0.49, folding endurance 770 ± 3 and maximum drug entrapment 98.12%. This result revealed that presence of propylene glycol (20% weight/weight of polymer) was used which gave good physicochem. properties and citric acid (0.2%weight/weight of polymer) was rapid disintegration of orodispersible film. Stability studies of the optimized batch H1 showed that there were no significant changes in appearance, elasticity, folding endurance, thickness, drug entrapment, tensile strength and in vitro disintegration time after storage at 40 ± 2°C and 75 ± 5%RH for a one month. This approach suggested that the orodispersible film of Hydroxyzine Hydrochloride using hydroxy Pr Me cellulose E15LV, citric acid and propylene glycol gave rapid disintegration of orodispersible film and provide faster onset of action. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3Quality Control 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. 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. 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 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride

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

Antihistamines and other prognostic factors for adverse outcome in hyperemesis gravidarum was written by Fejzo, Marlena S.;Magtira, Aromalyn;Schoenberg, Frederic Paik;MacGibbon, Kimber;Mullin, Patrick;Romero, Roberto;Tabsh, Khalil. And the article was included in European Journal of Obstetrics & Gynecology and Reproductive Biology in 2013.Product Details of 2192-20-3 This article mentions the following:

The purpose of this study is to determine the frequency of adverse perinatal outcome in women with hyperemesis gravidarum and identify prognostic factors. This is a case-control study in which outcomes of first pregnancies were compared between 254 women with hyperemesis gravidarum treated with i.v. fluids and 308 controls. Prognostic factors were identified by comparing the clin. profile of patients with hyperemesis gravidarum with a normal and an adverse pregnancy outcome. Binary responses were analyzed using either a Chi-square or Fisher exact test and continuous responses were analyzed using a t-test. Women with hyperemesis gravidarum have over a 4-fold increased risk of poor outcome including preterm birth and lower birth weight (p < 0.0001). Among maternal characteristics, only gestational hypertension had an influence on outcome (p < 0.0001). Treatment as an outpatient and/or by alternative medicine (acupuncture/acupressure/Bowen massage) was associated with a pos. outcome (p < 0.0089). Poor outcomes were associated with early start of symptoms (p < 0.019), and treatment with methylprednisolone (p < 0.0217), promethazine (p < 0.0386), and other antihistamines [diphenhydramine (Benadryl), dimenhydrinate (Gravol), doxylamine (Unisom), hydroxyzine (Vistaril/Atarax), doxylamine and pyridoxine (Diclectin/Bendectin)] (p < 0.0151) independent of effectiveness. Among these medications, only the other antihistamines were prescribed independent of severity: they were effective in less than 20% of cases and were taken by almost 50% of patients with an adverse outcome. Poor outcomes are significantly greater in women with HG and are associated with gestational hypertension, early symptoms, and antihistamine use. Given these results, there is an urgent need to address the safety and effectiveness of medications containing antihistamines in women with severe nausea of pregnancy. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3Product Details of 2192-20-3).

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 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.Product Details of 2192-20-3

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