Melekhin, A. O. et al. published their research in Food Chemistry in 2022 | CAS: 98105-99-8

6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 98105-99-8) belongs to piperazine derivatives. 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. 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).Safety of 6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid

Multi-class, multi-residue determination of 132 veterinary drugs in milk by magnetic solid-phase extraction based on magnetic hypercrosslinked polystyrene prior to their determination by high-performance liquid chromatography – tandem mass spectrometry was written by Melekhin, A. O.;Tolmacheva, V. V.;Goncharov, N. O.;Apyari, V. V.;Dmitrienko, S. G.;Shubina, E. G.;Grudev, A. I.. And the article was included in Food Chemistry in 2022.Safety of 6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid This article mentions the following:

A quant. multi-class multi-residue anal. method was developed for the determination of veterinary drugs in milk by high-performance liquid chromatog. – tandem mass spectrometry (HPLC-MS/MS). A total of 132 veterinary drugs investigated belonged to almost 15 classes including sulfonamides, 尾-lactams, tetracyclines, quinolones, macrolides, nitrofurans, nitroimidazoles, phenicols, lincosamides, pleuromutilins, macrocyclic lactones, quinoxaline antibiotics, benzimidazoles, anthelmintics, coccidiostats and some others. A magnetic solid-phase extraction procedure was developed using magnetic hypercrosslinked polystyrene (HCP/Fe3O4) for the sample preparation prior to HPLC-MS/MS without deproteinization step. The results indicated recoveries of 85-107% for 14 sulfonamides, 85-120% for 13 尾-lactams, 89-115% for 4 tetracyclines, 82-119% for 14 quinolones, 82-115% for 8 macrolides, 97-109% for 4 nitrofurans, 84-115% for 10 nitroimidazoles, 89-114% for 3 phenicols, 86-111% for 3 lincosamides, 97-102% for 2 pleuromutilins, 72-88% for 4 macrocyclic lactones, 87-104% for 4 quinoxaline antibiotics, 76-119% for 21 benzimidazoles, 79-115% for 12 anthelmintics, 81-118% for 12 coccidiostats and 75-119 % for 5 unclassified drugs, with relative standard deviations (RSDs) of less than 20%, and the LOQs ranged from 0.05 to 1 渭g kg-1. This methodol. was then applied to field-collected real milk samples and trace levels of some veterinary drugs were detected. In the experiment, the researchers used many compounds, for example, 6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 98105-99-8Safety of 6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid).

6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 98105-99-8) belongs to piperazine derivatives. 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. 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).Safety of 6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid

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

Zeidan, Tarek A. et al. published their research in Crystal Growth & Design in 2018 | CAS: 129722-25-4

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

Structural diversity of brexpiprazole and related analogues: Impact on solubility and drug delivery was written by Zeidan, Tarek A.;Tilak, Pranoti A.;Trotta, Jacob T.;Curran, Erin;Oliveira, Mark A.;Chiarella, Renato A.;Almarsson, Orn;Hickey, Magali B.. And the article was included in Crystal Growth & Design in 2018.Recommanded Product: 129722-25-4 This article mentions the following:

Brexpiprazole (BPZ) is an atypical antipsychotic drug indicated for the treatment of schizophrenia and depression. Crystal form screening of BPZ resulted in the formation of three polymorphs (I, II, and III), two methanol solvates, a toluene hemisolvate, and a dihydrate. Thermal anal. and solvent-mediated conversion experiments of the three unsolvated polymorphs established that Form I is the thermodynamically stable form at ambient temperature All three polymorphs are monotropically related, whereby Forms I and II are the most and least stable forms, resp. Structural diversity of BPZ was compared with two chem. related analogs, aripiprazole (APZ) and its active metabolite dehydro-aripiprazole (dAPZ). Like APZ and dAPZ, BPZ was shown to form a thermodynamically stable, hydrated crystal form when exposed to an aqueous environment; however, while APZ and dAPZ were characterized as monohydrates, BPZ is a dihydrate. The crystal structure of BPZ dihydrate (S2H2O) showed two water mols. connecting two BPZ mols., with hydrogen bonding occurring between both the piperazine nitrogen and the oxygen of the carbonyl moiety with different water mols. Despite the chem. similarity of BPZ, APZ, and dAPZ, comparison of all accumulated crystal structures reveals wide structural diversity, with a significant impact on physicochem. properties. In particular, the solubility of BPZ is significantly lower in water across the physiol. relevant pH range. Implications to drug delivery of these findings are discussed. 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: 129722-25-4Recommanded Product: 129722-25-4).

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

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

Wasana, Withanage Prasadini et al. published their research in Fish & Shellfish Immunology in 2022 | CAS: 85721-33-1

1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 85721-33-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Product Details of 85721-33-1

Probiotic effects of Pseudoalteromonas ruthenica: Antibacterial, immune stimulation and modulation of gut microbiota composition was written by Wasana, Withanage Prasadini;Senevirathne, Amal;Nikapitiya, Chamilani;Lee, Jong-Soo;Kang, Do-Hyung;Kwon, Kae Kyoung;Oh, Chulhong;De Zoysa, Mahanama. And the article was included in Fish & Shellfish Immunology in 2022.Product Details of 85721-33-1 This article mentions the following:

This study aimed to characterize and evaluate the probiotic properties of a newly isolated marine bacterium, strain S6031. The isolated strain was identified as Pseudoalteromonas ruthenica. In vivo experiments were conducted with P. ruthenica-immersed larvae and P. ruthenica-enriched Artemia fed to adult zebrafish. Disease tolerance of larval zebrafish against Edwardsiella piscicida was demonstrated by 66.34% cumulative per cent survival (CPS) in the P. ruthenica-exposed group, which was higher than the CPS of the control (46.67%) at 72 h post challenge (hpc). Heat-stressed larvae had 55% CPS in the P. ruthenica-immersed group, while the control had 30% CPS at 60 hpc. Immune-stress response gene transcripts (muc5.1, muc5.2, muc5.3, alpi2, alpi3, hsp70, and hsp90a) were induced, while pro-inflammatory genes (tnf伪, il1b, and il6) were downregulated in P. ruthenica-immersed larvae compared to the control. This trend was confirmed by low pro-inflammatory and high stress-responsive protein expression levels in P. ruthenica-exposed larvae. Adult zebrafish had higher CPS (27.2%) in the P. ruthenica-fed group than the control (9.52%) upon E. piscicida challenge, suggesting increased disease tolerance. Histol. anal. demonstrated modulation of goblet cell d. and average villus height in the P. ruthenica-supplemented group. Metagenomics anal. clearly indicated modulation of alpha diversity indexes and the relative abundance of Proteobacteria in the P. ruthenica-supplemented zebrafish gut. Furthermore, increased Firmicutes colonisation and reduced Bacteroidetes abundance in the gut were observed upon P. ruthenica supplementation. Addnl., this study confirmed the concentration-dependent increase of colony dispersion and macrophage uptake upon mucin treatment. In summary, P. ruthenica possesses remarkable functional properties as a probiotic that enhances host defense against diseases and thermal stress. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 85721-33-1Product Details of 85721-33-1).

1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 85721-33-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Product Details of 85721-33-1

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

Kashgari, Farzane Kuresh et al. published their research in Biomedicine & Pharmacotherapy in 2020 | CAS: 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. 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.Formula: C23H32N6O4S

Identification and experimental confirmation of novel cGMP efflux inhibitors by virtual ligand screening of vardenafil-analogues was written by Kashgari, Farzane Kuresh;Ravna, Aina;Sager, Georg;Lysaa, Roy;Enyedy, Istvan;Dietrichs, Erik Sveberg. And the article was included in Biomedicine & Pharmacotherapy in 2020.Formula: C23H32N6O4S This article mentions the following:

Background: Clin. studies have reported overexpression of PDE5 and elevation of intracellular cyclic GMP in various types of cancer cells. ABCC5 transports cGMP out of the cells with high affinity. PDE5 inhibitors prevent both cellular metabolism and cGMP efflux by inhibiting ABCC5 as well as PDE5. Increasing intracellular cGMP is hypothesized to promote apoptosis and growth restriction in tumor cells and also has potential for clin. use in treatment of cardiovascular disease and erectile dysfunction. Vardenafil is a potent inhibitor of both PDE5 and ABCC5-mediated cGMP cellular efflux. Nineteen novel vardenafil analogs that have been predicted as potent inhibitors by VLS were chosen for tests of their ability to inhibit ATP- dependent transport of cGMP by measuring the accumulation of cyclic GMP in inside-out vesicles. Aim: In this study, we investigated the ability of nineteen new compounds to inhibit ABCC5- mediated cGMP transport. We also determined the Ki values of the six most potent compounds Methods: Preparation of human erythrocyte inside out vesicles and transport assay. Results: Ki values for six of nineteen compounds that showed more than 50% inhibition of cGMP transport in the screening test were determined and ranged from 1.1 to 23.1渭M. One compound was significantly more potent than the pos. control, sildenafil. Conclusion: Our findings show that computational screening correctly identified vardenafil-analogs that potently inhibit cGMP efflux-pumps from cytosol and could have substantial clin. potential in treatment of patients with diverse disorders. 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: 224785-90-4Formula: C23H32N6O4S).

2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4) belongs to piperazine derivatives. 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.Formula: C23H32N6O4S

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

Rezaee, Michael E. et al. published their research in Journal of Sexual Medicine in 2020 | CAS: 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. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Recommanded Product: 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one

Are We Overstating the Risk of Priapism With Oral Phosphodiesterase Type 5 Inhibitors? was written by Rezaee, Michael E.;Gross, Martin S.. And the article was included in Journal of Sexual Medicine in 2020.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:

Priapism is an adverse drug reaction (ADR) associated with phosphodiesterase type 5 inhibitors (PDE5is) in the treatment of erectile dysfunction. The purpose of this study was to identify the true data about PDE5i-associated priapism to properly counsel patients. We queried the U.S. Food and Drug Administration (FDA) Adverse Reporting System Public Dashboard to identify cases of drug-induced priapism among medications commonly associated with priapism. Next, a systematic review and anal. of publications describing cases of drug-induced priapism were carried out. The main outome of this study is incidence of PDE5i-induced priapism.We found 411 cases of drug-induced priapism secondary to Viagra, Cialis, or Levitra reported to the Food and Drug Administration since 1998. Compared with PDE5is, drug-induced priapism was 2.6 (n = 1,065) and 2.0 times (n = 817) more commonly reported for second-generation antipsychotics and the antidepressant/sleep aid trazodone, resp. A total of 240 manuscripts describing cases of drug-induced priapism in patients with non-sickle cell disease were identified. PDE5i-induced priapism accounted for only 2.9% (n = 7) of drug-induced priapism cases. Second-generation antipsychotics (33.8%), a group of “other” medications (11.3%), and alpha-adrenergic antagonists (8.8%) accounted for the greatest percentage of published drug-induced priapism cases. Extensive counseling about priapism as an ADR for PDE5i for the routine treatment of erectile dysfunction is likely unnecessary. The study used national-level data to identify drug-induced priapism cases. Reported and published cases of drug-induced priapism may reflect more severe and atypical cases of this ADR, which may have underestimated our results.PDE5i-induced priapism is a rare event. Drug-induced priapism should be attributed to a wider spectrum of medications that can cause this condition.Rezaee ME, Gross MS. 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. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Recommanded Product: 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

Ding, Xiao et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2018 | CAS: 93643-24-4

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 93643-24-4

Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors was written by Ding, Xiao;Stasi, Luigi Piero;Ho, Ming-Hsun;Zhao, Baowei;Wang, Hailong;Long, Kai;Xu, Qiongfeng;Sang, Yingxia;Sun, Changhui;Hu, Huan;Yu, Haihua;Wan, Zehong;Wang, Lizhen;Edge, Colin;Liu, Qian;Li, Yi;Dong, Kelly;Guan, Xiaoming;Tattersall, F. David;Reith, Alastair D.;Ren, Feng. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.Product Details of 93643-24-4 This article mentions the following:

Inhibition of LRRK2 kinase activity with small mols. has emerged as a potential novel therapeutic treatment for Parkinson’s disease. Herein the authors disclose the discovery of a 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amine series as potent LRRK2 inhibitors identified through a kinase-focused set screening. Optimization of the physicochem. properties and kinase selectivity led to the discovery of compound 7 ((4-((4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone), which exhibited potent in vitro inhibition of LRRK2 kinase activity, good physicochem. properties and kinase selectivity across the kinome. Moreover, compound 7 was able to penetrate into the CNS, and in vivo pharmacol. studies revealed significant inhibition of Ser 935 phosphorylation in the brain of both rats (30 and 100 mg/kg) and mice (45 mg/kg) following oral administration. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Product Details of 93643-24-4).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 93643-24-4

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

Gao, Jennifer J. et al. published their research in Lancet Oncology in 2021 | CAS: 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. 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.COA of Formula: C23H30N8O

Overall survival in patients with hormone receptor-positive, HER2-negative, advanced or metastatic breast cancer treated with a cyclin-dependent kinase 4/6 inhibitor plus fulvestrant: a US Food and Drug Administration pooled analysis was written by Gao, Jennifer J.;Cheng, Joyce;Prowell, Tatiana M.;Bloomquist, Erik;Tang, Shenghui;Wedam, Suparna B.;Royce, Melanie;Krol, Danielle;Osgood, Christy;Ison, Gwynn;Sridhara, Rajeshwari;Pazdur, Richard;Beaver, Julia A.;Amiri-Kordestani, Laleh. And the article was included in Lancet Oncology in 2021.COA of Formula: C23H30N8O This article mentions the following:

Cyclin-dependent kinase 4/6 inhibitors (CDKIs) are oral targeted agents approved for use in combination with endocrine therapy as first-line or second-line treatment of patients with hormone receptor-pos., HER2-neg., advanced or metastatic breast cancer. We previously reported the pooled analyses of progression-free survival in patients in specific clinicopathol. subgroups, all of whom received consistent benefit from the addition of a CDKI to hormonal therapy. Here, we report the pooled overall survival results in patients treated with a CDKI and fulvestrant. In this exploratory anal., we pooled individual patient data from three phase 3 randomised trials of CDKI or placebo in combination with fulvestrant in patients with breast cancer submitted to the US Food and Drug Administration and approved before Aug 1, 2020, in support of marketing applications. All analyzed patients were aged at least 18 years, had an Eastern Cooperative Oncol. Group performance status of 0-1, had hormone receptor-pos., HER2-neg. advanced or metastatic breast cancer, and received at least one dose of CDKI or placebo in combination with fulvestrant. The median overall survival was estimated using Kaplan-Meier methods, and hazard ratios (HRs) with corresponding 95% CIs were estimated using Cox regression models. Patients were analyzed collectively, by number of previous lines of systemic endocrine therapy in any disease setting (first-line or endocrine naive vs second-line and later), and in various clinicopathol. subgroups of interest. The estimated median overall survival was not reported by group when the pooled population included patients treated across lines of therapy because of potential patient heterogeneity. All results presented are considered exploratory and hypothesis generating. Across the three pooled trials, 1960 patients were randomly assigned between Oct 7, 2013, and June 10, 2016 (12 patients were not treated and 1296 [66%] patients were randomly assigned to CDKI and 652 [33%] to placebo). In all treated patients (n = 1948), the estimated HR for overall survival was 0路77 (95% CI 0路68-0路88), with a median follow-up of 43路7 mo (IQR 37路 8-47路7) and deaths in 935 (48%) of the 1948 patients. The difference in estimated median overall survival was 7路 1 mo, favoring CDKIs. In patients who received CDKIs or placebo in combination with fulvestrant as first-line systemic endocrine therapy (two trials; n=396), the estimated HR for overall survival was 0路74 (95% CI 0路52-1路07), with a median follow-up of 39路4 mo (IQR 37路0-42路2). 123 (31%) of these patients died. The difference in estimated median overall survival could not be calculated because median overall survival was not estimable (95% CI 50路9-not estimable) in the CDKI group and was 45路7 mo (95% CI 41路7-not estimable) in the placebo group. In patients who received CDKIs or placebo in combination with fulvestrant as second-line or later systemic endocrine therapy (three trials; n=1552), the estimated HR for overall survival was 0路77 (95% CI 0路67-0路89), with a median follow-up of 45路1 mo (95% CI 39路2-48路5). 812 (52%) of these patients died. The difference in estimated median overall survival was 7路0 mo, favoring CDKIs. The addition of CDKIs to fulvestrant resulted in a consistent overall survival benefit in all pooled patients and within most clinicopathol. subgroups of interest. These findings support the existing standard of care of CDKIs plus fulvestrant for the treatment of patients with hormone receptor-pos., HER2-neg., advanced breast cancer.None. 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: 1211441-98-3COA of Formula: C23H30N8O).

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. 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.COA of Formula: C23H30N8O

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

Burchacka, Ewa et al. published their research in Biochimie in 2014 | CAS: 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 formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 27913-99-1

Substrate profiling of Finegoldia magna SufA protease, inhibitor screening and application to prevent human fibrinogen degradation and bacteria growth in vitro was written by Burchacka, Ewa;Sienczyk, Marcin;Frick, Inga-Maria;Wysocka, Magdalena;Lesner, Adam;Oleksyszyn, Jozef. And the article was included in Biochimie in 2014.Product Details of 27913-99-1 This article mentions the following:

SufA, which belongs to the subtilisin-like serine protease family, contains a non-canonical Asp-His-Ser catalytic triad. Under in vitro conditions, SufA is capable of human fibrinogen hydrolysis leading to inhibition of fibrin network formation, thus suggesting its important role in the development and progression of Finegoldia magna infections. In addition, it has been demonstrated that SufA can hydrolyze antibacterial peptides such as LL-37 and the chemokine MIG/CXCL 9, hence evading host defense mechanisms. Although the SufA protease from F. magna was discovered several years ago, its optimal substrate preference has not yet been identified. Considering the role of SufA, we have focused on the profiling of its substrate sequence preference spanning S1-S3 binding pockets using the FRET (fluorescence resonance energy transfer) approach. Next, based on the structure of the P1 residue of the developed substrate, we narrowed the inhibitor screening to the phosphonic analogs of amino acids containing an arginine-like side chain. Among all the compounds tested, only Cbz-6-AmNphthP(OPh)2 showed any inhibitory activity against SufA displaying k2/Ki value of 10 800 M-1 s-1. In addition, it prevented SufA-mediated human fibrinogen hydrolysis in vitro and exhibited potent antibacterial activity against F. magna, Staphylococcus aureus and Escherichia coli.Herein, we report on the substrate specificity, synthesis and kinetic evaluation of phosphonic inhibitors of SufA protease from F. magna which could help to establish its function in pathogenesis development and may lead to the elaboration of new antibacterial drugs. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1Product Details of 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 formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 27913-99-1

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

Patel, Kavitkumar N. et al. published their research in European Journal of Medicinal Chemistry in 2014 | CAS: 154590-34-8

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) 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.Formula: C15H20FN3O4

Design, synthesis and antitubercular evaluation of novel series of N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives was written by Patel, Kavitkumar N.;Telvekar, Vikas N.. And the article was included in European Journal of Medicinal Chemistry in 2014.Formula: C15H20FN3O4 This article mentions the following:

The analogs of N-[4-(piperazin-1-yl)phenyl]cinnamamide were designed and synthesized by a mol. hybridization approach in which part C of the designed mol. was linked through amide and carbamate functionality that improves the physicochem. properties and govern the pharmacokinetic and pharmacodynamic behavior. The systematic modification was done around the Part C to explore the structure activity relationship of antitubercular cinnamamides. All 52 compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis (M. tb) using Resazurin microtitre plate assay (REMA). Compound I with trifluoromethyl substitution exhibited good antitubercular activity of 3.125 渭g/mL. The synthesized N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives showed promising activity against M. tb. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8Formula: C15H20FN3O4).

tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate (cas: 154590-34-8) 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.Formula: C15H20FN3O4

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

Yin, Runting et al. published their research in Biochemical and Biophysical Research Communications in 2019 | CAS: 548472-68-0

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) 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.Computed Properties of C30H30Cl2N4O4

Dual specificity phosphatase (DUSP)-4 is induced by platelet-derived growth factor -BB in an Erk1/2-, STAT3- and p53-dependent manner was written by Yin, Runting;Eger, Glenda;Sarri, Niki;Rorsman, Charlotte;Heldin, Carl-Henrik;Lennartsson, Johan. And the article was included in Biochemical and Biophysical Research Communications in 2019.Computed Properties of C30H30Cl2N4O4 This article mentions the following:

Dual specificity phosphatase (DUSP) 4 has been described as a neg. regulator of MAP kinase signaling, in particular for the ERK1/2 and JNK pathways. We found that DUSP4 expression was upregulated in response to prolonged platelet-derived growth factor (PDGF)-BB stimulation. The PDGF-BB-induced DUSP4 expression was dependent on ERK1/2, STAT3 and p53. We found that inhibition of ERK1/2 effectively reduced DUSP4 mRNA levels, whereas STAT3 was necessary for maintaining p53 expression. P53 has binding sites in the DUSP4 promoter and was found to promote DUSP4 expression. In the experiment, the researchers used many compounds, for example, 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0Computed Properties of C30H30Cl2N4O4).

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) 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.Computed Properties of C30H30Cl2N4O4

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