Month: February 2023

Effects of tandospirone citrate and oxazolam on pharmacokinetics of valproic acid following oral administration of sodium valproate to rats was written by Hobara, Norio;Kameya, Hiromasa;Hokama, Nobuo;Ohshiro, Susumu;Hobara, Narumi;Sakanashi, Matao. And the article was included in Iryo Yakugaku in 2007.Quality Control of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate This article mentions the following:

The drug interactions between tandospirone citrate, a non-benzodiazepine antianxiety drug, and oxazolam, a minor benzodiazepine tranquilizer and antianxiety agent, and valproic acid (VPA), an anti-convulsant, were studied in rats. When tandospirone citrate or citric acid was administered orally immediately following oral administration (p.o.) of sodium valproate (VPA-Na), the plasma VPA levels were significantly lower than those in the control. In addition, pharmacokinetic parameters such as plasma VPA concentration and area under the plasma concentration-time curve up to 3 h (AUC) were significantly decreased. However, when tandospirone citrate was administered i.p., or both it and oxazolam were administered orally with VPA-Na, the VPA pharmacokinetic parameters were unchanged. These results suggest that decreases in plasma VPA concentrations (including those for AUC) may be due to a reduction in VPA-Na adsorption from the intestinal tract due to tandospirone citrate. In the experiment, the researchers used many compounds, for example, rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1Quality Control of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate).

rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Quality Control of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate

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

Photocatalysis as a tool for in vitro drug metabolism simulation: multivariate comparison of twelve metal oxides on a set of twenty model drugs was written by Gawlik, Maciej;Trawinski, Jakub;Skibinski, Robert. And the article was included in Catalysts in 2020.Synthetic Route of C23H32N6O4S This article mentions the following:

The constant development in the area of medicinal substances on the market and their subsequent progress in the field of drug anal. has become one of the reasons for the search for alternative, cheaper, and faster methods to determine the metabolism pathways of new mol. entities (NMEs). The simulation of transformation processes using photocatalysis is considered to be one of the promising methods. Although its effectiveness has been proven, the research has so far focused especially on titanium dioxide, while a more accurate comparison of the suitability of different photocatalysts in terms of their use in drug metabolism studies has not been performed. For this purpose, a set of twelve metal oxides was prepared and their photocatalytic efficiency in the direction of drug metabolism mimicking was checked on a model mixture of twenty medicinal substances differing both in chem. structure and pharmacol. properties. Incubation with human liver microsomes (HLMs) was used as the reference method. The metabolic profiles obtained with the use of LC-MS anal. were compared using multidimensional chemometric techniques; and the graphic presentation of the results in the form of PCA plot and cluster dendrogram enabled their detailed interpretation and discussion. All tested photocatalysts confirmed their effectiveness. However, the exact outcome of the study indicate advantage of the WO3-assisted photocatalysis over other metal oxides. 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. 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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C23H32N6O4S

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

The synthesis of piperazine-containing carbazole derivate and its sensing performance to proton was written by He, Yi;Li, Yan-mei. And the article was included in Fenzi Kexue Xuebao in 2011.Formula: C4H12Cl2N2 This article mentions the following:

A novel piperazine-containing carbazole derivative, N,N’-di[3-(N-carbazole)benzyl]-piperazine (DC-Pip) I, was designed and prepared The absorption and fluorescence maxima of DC-Pip were observed at 300 and 405 nm, resp. DC-Pip emits strong blue fluorescence and has a high quantum yield (桅_F = 0.94) in solution, which indicates that DC-Pip can be used as fluorescence emitting materials. The effect of pH on the fluorescence characteristics of DC-Pip in H₂O/DMF (4:1, V/V) solution has also been investigated, the intensity of fluorescence decreases with the decrease of pH value, these results shows that DC-Pip offers potential as optical sensor for protons. In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3Formula: C4H12Cl2N2).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.Formula: C4H12Cl2N2

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

Pharmaceuticals and personal care products in the seawater around a typical subtropical tourist city of China and associated ecological risk was written by Chen, Hongzhe;Chen, Wenfeng;Guo, Huige;Lin, Hui;Zhang, Yuanbiao. And the article was included in Environmental Science and Pollution Research in 2021.Formula: C20H17F2N3O3 This article mentions the following:

Pharmaceuticals and personal care products (PPCPs) in the sea area surrounding a densely populated tourist city in southeastern China were investigated. In total, 32 PPCP pollutants classified into 23 categories were detected. Different spatial distribution patterns of PPCPs indicated possible contamination from runoff and multiple local sources. The labile-to-conservative ratios of PPCPs showed the influence of untreated domestic sewage. In addition, increased concentrations of ciprofloxacin, enrofloxacin, and erythromycin around aquaculture farms imply that aquaculture cannot be neglected as a source. The concentrations of oxytetracycline, ranitidine, ciprofloxacin, miconazole, and sulfamethizole were higher in the wet season than those in the dry season, and the difference in pharmaceutical consumption was suspected to be the main driving factor of this seasonal variation. The risk quotients calculated with the maximum concentrations of miconazole, triclosan, dehydronifedipine, and triclocarban exceeded 0.1, indicating potential moderate or high risks. Antibacterial agents in daily chems. and azole broad-spectrum antifungals were associated with the highest risks in this study; this might be another significant pollution characteristic in the sea area around this subtropical tourist city. 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: 98105-99-8Formula: C20H17F2N3O3).

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. 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.Formula: C20H17F2N3O3

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

Green methodologies in organic synthesis: microwave-assisted study on carbostyril derivatives under phase transfer catalysis was written by Kollapudi, Chandra Babu;Gutta, Madhusudhan;Reguri, Buchi Reddy. And the article was included in Heterocyclic Letters in 2015.Reference of 129722-25-4 This article mentions the following:

In this paper few carbostyril derivatives were synthesized by microwave method as well as by green chem. method. By applying the green synthesis method, not only avoided the use of DDQ and benzyl halide which is hazardous but also the formation of by products. The quaternary ammonium salts (PTC) under microwave conditions towards Aripiprazole (carbostyril derivative) act as a reagent and gave dehydrogenated and benzylated carbostyril from 3,4-dihydro carbostyril derivatives 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: 129722-25-4Reference 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. 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).Reference of 129722-25-4

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

Development of a multicomponent immunochromatographic test system for the detection of fluoroquinolone and amphenicol antibiotics in dairy products was written by Hendrickson, O. D.;Zvereva, E. A.;Shanin, I. A.;Zherdev, A. V.;Dzantiev, B. B.. And the article was included in Journal of the Science of Food and Agriculture in 2019.Computed Properties of C19H20F3N3O3 This article mentions the following:

BACKGROUND : Ciprofloxacin (CIP) and chloramphenicol (CAP) are relevant antibiotics of the fluoroquinolone (FQ) and amphenicol (AP) groups, resp., widely used in veterinary practice and they contaminate agricultural products. In this study, a rapid and sensitive immunochromatog. assay (ICA) was developed for simultaneous detection of CIP and CAP in dairy products. The ICA was carried out in a direct competitive format using gold nanoparticles as a label. RESULTS : The ICA developed here allowed for the detection of CIP and CAP in Triton X-100-containing buffered saline (PBST) within 15 min with instrumental detection limits of 20 pg mL^-1 and 0.5 ng mL^-1, resp., and with a visual detection limit of 5 ng mL^-1 for both antibiotics. The ICA showed cross-reactivity (69-160%) to 19 antibiotics in the FQ group and no cross-reactivity (<0.1%) to 2 antibiotics of the AP group. The ICA allowed detection of CIP and CAP in a panel of dairy products by employing a simple procedure of preliminary sample preparation The detection limits for the two antibiotics were the same as in PBST. The anal. recoveries of CIP and CAP in dairy products ranged from 83% to 120%. CONCLUSION : The anal. characteristics of the test system allow its use for the detection of antibiotics in milk and dairy products during all steps of production 漏 2019 Society of Chem. Industry. 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. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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).Computed Properties of C19H20F3N3O3

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

Expression of MDM2 in macrophages promotes the early postentry steps of HIV-1 infection through inhibition of p53 was written by Breton, Yann;Desrosiers, Vincent;Ouellet, Michel;Deshiere, Alexandre;Torresilla, Cynthia;Cohen, Eric A.;Tremblay, Michel J.. And the article was included in Journal of Virology in 2019.Application In Synthesis of 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one This article mentions the following:

The mol. basis for HIV-1 susceptibility in primary human monocyte-derived macrophages (MDMs) was previously evaluated by comparing the transcriptome of infected and bystander populations. In this study, MDM2 silencing through transcript-specific small interfering RNAs in MDMs induced a reduction in HIV-1 reverse transcription and integration along with an increase in the expression of p53-induced genes, including CDKN1A. Experiments with Nutlin-3, a pharmacol. inhibitor of MDM2 p53-binding activity, showed a similar effect on HIV-1 infection, suggesting that the observed restriction in HIV-1 production results from the release/activation of p53 and not the absence of MDM2 per se. IMPORTANCE Macrophages, with their long life span in vivo and their resistance to HIV-1-mediated cytopathic effect, might serve as viral reservoirs, contributing to virus persistence in an infected individual. Identification of host factors that increase the overall susceptibility of macrophages to HIV-1 might provide new therapeutic targets for the efficient control of viral replication in these cells and limit the formation of reservoirs in exposed individuals. In this study, we demonstrate the importance of p53 regulation by MDM2, which creates a cellular environment more favorable to the early steps of HIV-1 replication. Moreover, we show that p53 stabilization reduces virus infection in human macrophages, highlighting the important role of p53 in antiviral immunity. 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: 548472-68-0Application In Synthesis of 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one).

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. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Application In Synthesis of 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one

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

FGFR2 fusion proteins drive oncogenic transformation of mouse liver organoids towards cholangiocarcinoma was written by Cristinziano, Giulia;Porru, Manuela;Lamberti, Dante;Buglioni, Simonetta;Rollo, Francesca;Amoreo, Carla Azzurra;Manni, Isabella;Giannarelli, Diana;Cristofoletti, Cristina;Russo, Giandomenico;Borad, Mitesh J.;Grazi, Gian Luca;Diodoro, Maria Grazia;Giordano, Silvia;Sacconi, Andrea;Forcato, Mattia;Anastasi, Sergio;Leonetti, Carlo;Segatto, Oreste. And the article was included in Journal of Hepatology in 2021.Application of 872511-34-7 This article mentions the following:

About 15% of intrahepatic cholangiocarcinomas (iCCAs) express fibroblast growth factor receptor 2 (FGFR2) fusion proteins (FFs), usually alongside mutational inactivation of TP53, CDKN2A or BAP1. In FFs, FGFR2 residues 1-768 fuse to sequences encoded by a diverse array of partner genes (>60) causing oncogenic FF activation. While FGFR-specific tyrosine kinase inhibitors (F-TKI) provide clin. benefit in FF+ iCCA, responses are partial and/or limited by resistance mechanisms, such as the V565F substitution in the FGFR2 gatekeeper residue. Improving on FF targeting in iCCA therefore remains a critical unmet need. Herein, we aimed to generate a murine model of FF-driven iCCA and use this to uncover actionable FF-associated dependencies.Four iCCA FFs carrying different fusion sequences were expressed in Tp53-/- mouse liver organoids. Tumorigenic properties of genetically modified liver organoids were assessed by transplantation into immuno-deficient mice. Cellular models derived from neoplastic lesions were exploited for pre-clin. studies.Transplantation of FF-expressing liver organoids yielded tumors diagnosed as CCA based on histol., phenotypic and transcriptomic analyses. The penetrance of this tumorigenic phenotype was influenced by FF identity. Tumor organoids and 2D cell lines derived from CCA lesions were addicted to FF signaling via Ras-Erk, regardless of FF identity or V565F mutation. Dual blockade of FF and the Ras-Erk pathway by concomitant pharmacol. inhibition of FFs and Mek1/2 provided greater therapeutic efficacy than single agent F-TKI in vitro and in vivo.FF-driven iCCA pathogenesis was successfully modeled on a Tp53-/- murine background, revealing biol. heterogeneity among structurally different FFs. Double blockade of FF-ERK signaling deserves consideration for precision-based approaches against human FF+ iCCA.Intrahepatic cholangiocarcinoma (iCCA) is a rare cancer that is difficult to treat. A subtype of iCCA is caused by genomic alterations that generate oncogenic drivers known as FGFR2 fusions. Patients with FGFR2 fusions respond to FGFR inhibitors, but clin. responses are often of modest duration. We used animal and cellular models to show that FGFR2 fusions require the activity of a downstream effector named Mek1/2. We found that dual blockade of FGFR2 fusions and Mek1/2 was more effective than isolated inhibition of FGFR2 fusions, pointing to the potential clin. utility of dual FGFR2-MEK1/2 blockade in patients with iCCA. 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: 872511-34-7Application of 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. Simple N-substituted piperazines have been found in many drug molecules. 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. Application of 872511-34-7

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

Comparative evaluation of efficacies of dl-tetramisole and piperazine against Ascaridia galli in chickens was written by Altaif, K. I.. And the article was included in American Journal of Veterinary Research in 1972.Formula: C4H12Cl2N2 This article mentions the following:

Dl-tetramisole (I) [5036-02-2] (20 and 40 mg/kg) administered in drinking water proved 87.7 and 99.0% efficacious, resp., against mature Ascaridia galli in chickens, whereas 20 mg/kg I mixed with feed gave a 63.0% reduction of the fecal egg count. Piperazine-2HCl [142-64-3] (260 mg/kg) given in drinking water resulted in a 96.4% reduction in fecal egg count whereas when given in the feed a 79.0% reduction was observed In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3Formula: C4H12Cl2N2).

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.Formula: C4H12Cl2N2

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

Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation was written by Mishra, Chandra Bhushan;Kumari, Shikha;Angeli, Andrea;Bua, Silvia;Tiwari, Manisha;Supuran, Claudiu T.. And the article was included in Journal of Medicinal Chemistry in 2018.HPLC of Formula: 27469-60-9 This article mentions the following:

Two series of novel benzenesulfonamide derivatives were synthesized and evaluated for their human carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity against four isoforms, hCA I, hCA II, hCA VII, and hCA IX. It was found that compounds of both series showed low to medium nanomolar inhibitory potential against all isoforms. Some of these derivatives displayed selective inhibition against the epileptogenesis related isoforms hCA II and VII, within the nanomolar range. These potent hCA II and VII inhibitors were evaluated as anticonvulsant agents against MES and s.c.-PTZ induced convulsions. These sulfonamides effectively abolished induced seizures in both models. Furthermore, time dependent seizure protection capability of the most potent compound I was also evaluated. A long duration of action was displayed, with efficacy up to 6 h after drug administration. The compound appeared as an orally active anticonvulsant agent without showing neurotoxicity in a rotarod test, a nontoxic chem. profile being observed in subacute toxicity study. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9HPLC of Formula: 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.HPLC of Formula: 27469-60-9

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