Heterocyclic Building Blocks-piperidine

N-Substituted homopiperazine barbiturates as gelatinase inhibitors was written by Wang, Jun;Medina, Carlos;Radomski, Marek W.;Gilmer, John F.. And the article was included in Bioorganic & Medicinal Chemistry in 2011.Safety of 1-(1,4-Diazepan-1-yl)ethanone This article mentions the following:

Matrix metalloproteinases are implicated in a wide range of pathophysiol. processes and potent selective inhibitors for these enzymes continue to be eagerly sought. 5,5-Disubstituted barbiturates hold promise as inhibitor types being stable in vivo and relatively selective for the gelatinases (MMP-2 and MMP-9). In this paper we describe the synthesis of 5-piperazine and -homopiperazine substituted barbiturates. The activity of these compounds as gelatinase inhibitors was evaluated using supernatants from 12-O-tetradecanoylphorbol-13-acetate (PMA)-stimulated HT-1080 cells as well as using recombinant human MMPs. N-Acyl homopiperazine compounds were found to be potent inhibitors of the gelatinases (range in nM) and generally more potent than the corresponding piperazine analogs. The panel of N-acyl homopiperazines was enlarged in order to exploit differences between the gelatinases at the S2′ site in order to design MMP-2- or MMP-9-selective inhibitors. Compounds in this group exhibited single digit nano-molar potency and some selectivity between the two enzymes. Representative potent compounds were effective inhibitors of cancer cell migration. In the experiment, the researchers used many compounds, for example, 1-(1,4-Diazepan-1-yl)ethanone (cas: 61903-11-5Safety of 1-(1,4-Diazepan-1-yl)ethanone).

1-(1,4-Diazepan-1-yl)ethanone (cas: 61903-11-5) 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.Safety of 1-(1,4-Diazepan-1-yl)ethanone

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

A quadruple-labeling luminescence strategy for multiplexed immunoassay of 51 drugs in milk with an automated pretreatment system was written by Zhang, Yaqing;Chang, Xiaoxi;Wang, Xin;Tao, Xiaoqi. And the article was included in Analytical Methods in 2019.Computed Properties of C19H20F3N3O3 This article mentions the following:

In this study, a novel combination of quadruple-labeling luminescence strategy multiplexed immunoassay (QLL-MIA) and an automated pretreatment system for simultaneous extraction and determination of 20 fluoroquinolones (FQs), 15 β-lactams, 15 sulfonamides (SAs), and chloramphenicol (CAP) in milk was developed. The strategy integrated 2 fluorescence probes, and 2 chemiluminescence probes to achieve signal separation, and a new combination of a nucleic acid extraction system and immunomagnetic beads (IMBs) as the automated pretreatment system to achieve simultaneous determination of 51 drugs. Taking advantage of automated pretreatment system for concentrating milk sample with 5 times and saving the extraction time, the limits of detection (LODs) for FQs, β-lactams, SAs, and CAP in the QLL-MIA range from 29.1 ng L^-1 for ciprofloxacin (CIP) to 8000.0 ng L^-1 (8.0μg L^-1) for trovafloxacin (TRO), 20.0 ng L^-1 for ceftiofur (CEF) to 3409.1 ng L^-1 (3.4μg L^-1) for cephalexin (CEL), 8.6 ng L^-1 for sulfadimethoxine (SDM) to 328.2 ng L^-1 (0.3μg L^-1) for sulfadiazine (SDZ), and 6.0 ng L^-1 for CAP. The recoveries ranged from 80.6% to 105.5% at a fortified concentration of LOD and 2 LOD, with a coefficient of variation <15%. Anal. of field milk samples by the combination of QLL-MIA and the automated pretreatment system (the developed QLL-MIA) was in accordance with that of liquid chromatog. coupled with tandem mass spectrometry (LC-MS/MS). The above results demonstrated that the developed QLL-MIA could simultaneously screen trace amounts of FQs, β-lactams, SAs, and CAP in field samples, suitable for high-throughput screening of low-mol. weight contaminants. 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: 113617-63-3Computed Properties of C19H20F3N3O3).

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. 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.Computed Properties of C19H20F3N3O3

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

Comparative studies of emesis in pigeons and dogs was written by Koster, Rudolf. And the article was included in Journal of Pharmacology and Experimental Therapeutics in 1957.Recommanded Product: Piperazine Dihydrochloride This article mentions the following:

Comparative studies of emesis were made in pigeons and dogs by using the emetic drugs apomorphine, CuSO₄, and piperazine-HCl, and the antiemetic drugs cyclizine, atropine, scopolamine, and chlorpromazine in various dosages and combinations. Emetic, antiemetic, and other effects are reported, and the possible mechanisms of action are discussed. In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3Recommanded Product: Piperazine Dihydrochloride).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine is 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.Recommanded Product: Piperazine Dihydrochloride

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

Keeping up with the guidelines: design changes to the STREAM stage 2 randomised controlled non-inferiority trial for rifampicin-resistant tuberculosis was written by Goodall, Ruth L.;Sanders, Karen;Bronson, Gay;Gurumurthy, Meera;Torrea, Gabriela;Meredith, Sarah;Nunn, Andrew;Rusen, I. D.;on behalf of the STREAM Trial Team. And the article was included in Trials in 2022.Safety of 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins This article mentions the following:

Results from the STREAM stage 1 trial showed that a 9-mo regimen for patients with rifampicin-resistant tuberculosis was non-inferior to the 20-mo regimen recommended by the 2011 WHO treatment guidelines. Similar levels of severe adverse events were reported on both regimens suggesting the need for further research to optimize treatment. Stage 2 of STREAM evaluates two addnl. short-course regimens, both of which include bedaquiline. Throughout stage 2 of STREAM, new drug choices and a rapidly changing treatment landscape have necessitated changes to the trial’s design to ensure it remains ethical and relevant. This paper describes changes to the trial design to ensure that stage 2 continues to answer important questions. These changes include the early closure to recruitment of two trial arms and an adjustment to the definition of the primary endpoint. If the STREAM exptl. regimens are shown to be non-inferior or superior to the stage 1 study regimen, this would represent an important contribution to evidence about potentially more tolerable and more efficacious MDR-TB regimens, and a welcome advance for patients with rifampicin-resistant tuberculosis and tuberculosis control programs globally. In the experiment, the researchers used many compounds, for example, 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1Safety of 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins).

8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Safety of 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins

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

Glutathione. X. Human erythrocyte membrane diffusion coefficients for diazene derivatives of the DIP [diazenedicarboxylic acid bis(N’-methylpiperazide)] series via intracellular thiol oxidation was written by Kosower, Nechama S.;Kosower, Edward M.;Saltoun, Gilda;Lev, Lilly. And the article was included in Biochemical and Biophysical Research Communications in 1975.Reference of 5308-28-1 This article mentions the following:

The thiol-oxidizing agent, DIP and its homologs with different N’-alkyl groups can be used to obtain membrane diffusion coefficients for human erythrocytes at 1°. From the initial rates of intracellular glutathione oxidation and the 2-octanol partition coefficients for the specific DIP homolog, diffusion coefficients of ∼1 × 10-8 cm2/sec were observed The method (irreversible loss of permeant through well-defined intracellular reaction) may be used to evaluate membrane properties and possibly for the study of substituent effects on drug entry into cells. In the experiment, the researchers used many compounds, for example, 1-Isobutylpiperazine (cas: 5308-28-1Reference of 5308-28-1).

1-Isobutylpiperazine (cas: 5308-28-1) 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.Reference of 5308-28-1

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

Combination therapy with topical alprostadil and phosphodiesterase-5 inhibitors after failure of oral therapy in patients with erectile dysfunction: a prospective, two-arm, open-label, non-randomized study was written by Garrido-Abad, Pablo;Senra-Bravo, Isabel;Manfredi, Celeste;Fernandez-Pascual, Esau;Linares-Espinos, Estefania;Fernandez-Arjona, Manuel;Varillas-Delgado, David;Martinez-Salamanca, Juan Ignacio. And the article was included in International Journal of Impotence Research in 2022.Synthetic Route of C23H32N6O4S This article mentions the following:

Abstract: To evaluate efficacy and safety of combination therapy with PDE5I and topical alprostadil in patients with ED non-responders to PDE5I alone. Patients over 18 years old, with stable sexual relationship for at least 6 mo, and ED non-responders to PDE5I monotherapy were included in study. At baseline the variables assessed were 5-item version of International Index of Erectile Function (IIEF-5), and Sexual Encounter Profile Questions 2 and 3 (SEP-2 and SEP-3). All patients were assigned to monotherapy group (Group A) or combination therapy group (Group B) based on their preference. 52 patients were previously treated with sildenafil 100 mg (30.6%), 6 with vardenafil 20 mg (3.5%), 56 with tadalafil 20 mg (32.9%), and 56 with avanafil 200 mg (32.9%). Mean IIEF-5 score increased significantly in Group B after treatment compared to baseline, conversely patients in Group A showed no increase. Number of affirmative responses to SEP-2 was higher after treatment compared to baseline only in Group B. Number of affirmative responses to SEP-3 was higher after treatment compared to baseline in both groups (p < 0.001). Number of affirmative responses to GAQ-Q1 and GAQ-Q2 was significantly higher in Group B compared to Group A (p < 0.001). A total of 59 (34.7%) patients experienced AEs. No episode of priapism was recorded. Combination therapy with topical alprostadil and PDE5I seems to be more effective than topical alprostadil alone without worsening safety of the treatment. 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: 224785-90-4Synthetic Route of 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. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Synthetic Route of C23H32N6O4S

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

Extractive-spectrophotometric determination of phenothiazine derivatives as compounds with picramic acid was written by Puzanowska-Tarasiewicz, Helena;Regulska, Ewa;Kleszczewska, Ewa. And the article was included in Acta Poloniae Pharmaceutica in 1990.Product Details of 316-81-4 This article mentions the following:

Promazine, chlorpromazine, and thioproperazine were extracted from. aqueous solutions with a CHCl₃ solution of picramic acid as 1:1 associates The drugs were determined in the extracts by spectrophotometry at 500 nm in concentrations of 8-80, 25-250, and 16-160 μg/mL concentrations, resp. The average error did not exceed 1.12%. 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: 316-81-4Product Details of 316-81-4).

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. 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 316-81-4

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

Modeling glioma with human embryonic stem cell-derived neural lineages was written by Modrek, Aram S.;Prado, Jod;Bready, Devin;Dhaliwal, Joravar;Golub, Danielle;Placantonakis, Dimitris G.. And the article was included in Methods in Molecular Biology (New York, NY, United States) in 2018.Product Details of 1062368-24-4 This article mentions the following:

Gliomas are malignant primary tumors of the central nervous system. Their cell-of-origin is thought to be a neural progenitor or stem cell that acquires mutations leading to oncogenic transformation. Thanks to advances in human stem cell biol., it has become possible to derive human cell types that represent putative cells-of-origin in vitro and model the gliomagenesis process by systematically introducing genetic alterations in these human cells. Here, we present methods to derive human neural stem cells (NSCs) from human embryonic stem cells (hESCs). Because these NSCs are genetically unmodified at baseline, they can be used as a cellular platform to study the effects of individual oncogenic hits in a well-controlled manner in the backdrop of a human genetic background. We also present some key applications of these NSCs, which include their transduction with lentiviral vectors, their neuroglial differentiation and xenografting methods into immunocompromised mice to assess in vivo behavior. 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: 1062368-24-4Product Details of 1062368-24-4).

4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1062368-24-4) 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 1062368-24-4

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

Effects of different pediatric drugs on the color stability of various restorative materials applicable in pediatric dentistry was written by Tuzuner, Tamer;Turgut, Sedanur;Baygin, Ozgul;Yilmaz, Nagehan;Tuna, Elif Bahar;Ozen, Bugra. And the article was included in BioMed Research International in 2017.Formula: C21H29Cl3N2O2 This article mentions the following:

The chronic recommendation of pediatric drugs could exhibit erosive and cariogenic problems. To evaluate the effects of different pediatric drugs on the color stability of various restorative materials. Five specimens (1 mm × 3 mm) were prepared and immersed in ten different pediatric drugs and agitated every 8 h daily for 2 min up to 1 wk. Between immersion periods, the samples were stored in artificial saliva. After 1-wk period, ΔE* values were calculated Two-way ANOVA and Fisher’s LSD test were used for statistical anal. at a level of p < 0.05. Results. ΔE* values were only significantly influenced by restorative material factor (p < 0.001) and varied in the range of 2.08 and 6.55 units for all drugs/restorative materials. The highest ΔE* was found in Ferrosanol B-composite (6.55 ± 1.38) and the lowest one was found in Dolven-glass ionomer (2.08 ± 0.40) pairwise. The most prominent ΔE* value elevations were obtained in composite material compared to the compomer and/or glass ionomers in Macrol, Ferrosanol B, and Ventolin (p < 0.001; for all) and also for other drugs (p < 0.05). Dolven exhibited significantly higher values compared to Augmentin (p = 0.021), Macrol (p = 0.018), and Ventolin (p = 0.013) in compomer group. The clin. perceptible color changes for tested composite/pediatric drug pairwise can be more problematic than compomer and glass ionomers in pediatric dentistry. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3Formula: C21H29Cl3N2O2).

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 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.Formula: C21H29Cl3N2O2

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

Oxidative Aromatization of 3,4-Dihydroquinolin-2(1H)-ones to Quinolin-2(1H)-ones Using Transition-Metal-Activated Persulfate Salts was written by Chen, Weiming;Sun, Changliang;Zhang, Yan;Hu, Tianwen;Zhu, Fuqiang;Jiang, Xiangrui;Abame, Melkamu Alemu;Yang, Feipu;Suo, Jin;Shi, Jing;Shen, Jingshan;Aisa, Haji A.. And the article was included in Journal of Organic Chemistry in 2019.Product Details of 129722-25-4 This article mentions the following:

Inorganic persulfate salts were identified as efficient reagents for the oxidative aromatization of 3,4-dihydroquinolin-2(1H)-ones through the activation of readily available transition metals, such as iron and copper. The feasible protocol conforming to the requirement of green chem. was utilized in the preparation of the key intermediate 7-(4-chlorobutoxy)quinolin-2(1H)-one of brexpiprazole in 80% isolated yield on a 100 g scale, and different quinolin-2(1H)-one derivatives with various functional groups were demonstrated in 52-89% yields. 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: 129722-25-4Product Details of 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. 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.Product Details of 129722-25-4

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