Month: November 2022

Fujimoto, Shota’s team published research in Journal of Gastroenterology and Hepatology in 36 | CAS: 863127-77-9

Journal of Gastroenterology and Hepatology published new progress about 863127-77-9. 863127-77-9 belongs to piperazines, auxiliary class TGF-beta/Smad,Bcr-Abl,Natural product, name is N-(2-Chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide hydrate, and the molecular formula is C22H28ClN7O3S, SDS of cas: 863127-77-9.

Fujimoto, Shota published the artcileIndocyanine green-labeled dasatinib as a new fluorescent probe for molecular imaging of gastrointestinal stromal tumors, SDS of cas: 863127-77-9, the publication is Journal of Gastroenterology and Hepatology (2021), 36(5), 1253-1262, database is CAplus and MEDLINE.

It is difficult to differentiate gastrointestinal stromal tumors (GISTs) from other subepithelial lesions under gastrointestinal endoscopy. Because most GISTs express tyrosine kinase receptor c-KIT, fluorescence-labeled c-KIT-specific tyrosine kinase inhibitors seem to be useful agents for mol. imaging of GIST. We aimed to develop a near-IR fluorescent imaging technol. for GIST targeting c-KIT using the novel fluorescent probe indocyanine green-labeled dasatinib (ICG-dasatinib) and to investigate the antitumor effect of ICG-dasatinib on GIST cells. Indocyanine green-labeled dasatinib was synthesized by labeling linker-induced dasatinib with ICG derivative 3-indocyanine-green-acyl-1,3-thiazolidine-2-thione. Human GIST cell lines GIST-T1 and GIST-882M were incubated with ICG-dasatinib and observed by fluorescent microscopy. GIST cells were incubated with ICG-dasatinib, unlabeled dasatinib, or imatinib, and cell viabilities were evaluated. S.c. GIST model mice or orthotopic GIST model rats were i.v. injected with ICG-dasatinib and observed using an IVIS Spectrum. Strong fluorescent signals of ICG-dasatinib were observed in both GIST cell lines in vitro. IC50 values for ICG-dasatinib, unlabeled dasatinib, and imatinib were 13.9, 1.17, and 16.2 nM in GIST-T1 and 26.6, 3.63, and 47.6 nM in GIST-882M cells, resp. ICG-dasatinib accumulated in s.c. xenografts in mice. Fluorescent signals were also observed in liver and gallbladder, indicating biliary excretion; however, fluorescence intensity of tumors was significantly higher than that of intestine after washing. Strong fluorescent signals were observed in orthotopic xenografts through the covering normal mucosa in rats. Indocyanine green-labeled dasatinib could visualize GIST cells and xenografted tumors. The antitumor effect of ICG-dasatinib was preserved to the same degree as imatinib.

Journal of Gastroenterology and Hepatology published new progress about 863127-77-9. 863127-77-9 belongs to piperazines, auxiliary class TGF-beta/Smad,Bcr-Abl,Natural product, name is N-(2-Chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide hydrate, and the molecular formula is C22H28ClN7O3S, SDS of cas: 863127-77-9.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Hu, Feng’s team published research in European Journal of Medicinal Chemistry in 213 | CAS: 67914-60-7

European Journal of Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Synthetic Route of 67914-60-7.

Hu, Feng published the artcile18F-labeled radiotracers for in vivo imaging of DREADD with positron emission tomography, Synthetic Route of 67914-60-7, the publication is European Journal of Medicinal Chemistry (2021), 113047, database is CAplus and MEDLINE.

Designer Receptors Exclusively Activated by Designer Drugs (DREADD) are a preclin. chemogenetic approach with clin. potential for various disorders. In vivo visualization of DREADDs has been achieved with positron emission tomog. (PET) using 11C radiotracers. The objective of this study was to develop DREADD radiotracers labeled with 18F for a longer isotope half-life. A series of non-radioactive fluorinated analogs of clozapine with a wide range of in vitro binding affinities for the hM3Dq and hM4Di DREADD receptors has been synthesized for PET. Compound [18F]7b was radiolabeled via a modified 18F-deoxyfluorination protocol with a com. ruthenium reagent. [18F]7b demonstrated encouraging PET imaging properties in a DREADD hM3Dq transgenic mouse model, whereas the radiotracer uptake in the wild type mouse brain was low. [18F]7b is a promising long-lived alternative to the DREADD radiotracers [11C]clozapine ([11C]CLZ) and [11C]deschloroclozapine ([11C]DCZ).

European Journal of Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Synthetic Route of 67914-60-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Geng, Lingjun et al. published their research in Microchemical Journal in 2022 | CAS: 70458-96-7

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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.Name: 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid

Molecularly imprinted electrochemical sensor based on multi-walled carbon nanotubes for specific recognition and determination of chloramphenicol in milk was written by Geng, Lingjun;Huang, Jingcheng;Zhai, Hongguo;Shen, Zheng;Han, Jie;Yu, Yanyang;Fang, Honggang;Li, Falan;Sun, Xia;Guo, Yemin. And the article was included in Microchemical Journal in 2022.Name: 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid The following contents are mentioned in the article:

A molecularly imprinted electrochem. sensor of chloramphenicol (CAP) with high sensitivity and good selectivity is introduced in this paper. Glassy carbon electrode (GCE) was modified by chitosan-multiwalled carbon nanotubes (CS-MWCNTs), the CS could improve the dispersion of MWCNTS, and the MWCNTS could significantly improve the current response of the sensor, thus improving the sensitivity. CAP was used as a template mol. and o-phenylenediamine (o-PD) was used as a functional monomer, resp. Molecularly imprinted polymers (MIPs) were prepared on the surface of a GCE modified with CS-MWCNTs by electro-polymerization The MIPs provided specific recognition sites for the detection of chloramphenicol. The exptl. parameters such as polymerization cycle, concentration ratio of template mol. to functional monomer, supporting electrolyte pH and incubation time were optimized. Under optimized exptl. conditions, the sensor has a linear range of 0.1-1000 ng/mL and the limit of detection (LOD) of 3.3 x 10-2 ng/mL (S/N = 3). The sensor had high selectivity, good stability and reproducibility for the detection of CAP, and it has been successfully used for the determination of CAP in real spiked milk samples. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Name: 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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.Name: 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid

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

Kaur, Tanvir et al. published their research in Archives of Microbiology in 2022 | CAS: 70458-96-7

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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. 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. COA of Formula: C16H18FN3O3

Biosynthesis of zinc oxide nanoparticles via endophyte Trichodermaviride and evaluation of their antimicrobial and antioxidant properties was written by Kaur, Tanvir;Bala, Manju;Kumar, Gaurav;Vyas, Ashish. And the article was included in Archives of Microbiology in 2022.COA of Formula: C16H18FN3O3 The following contents are mentioned in the article:

The biogenic method for synthesis of nanoparticles is preferred over the traditional strategies, on account of its ease, environmental friendliness, and cost-effectivity, wherein fungi endorse themselves to be the most appropriate precursor for the same. In recent times numerous metal nanoparticles have been reported to exhibit significant therapeutic activities, out of which Zinc Oxide nanoparticles (ZnO NPs) stand apart on account of their multidimensional nature. Thus, this study was carried out with an aim to biosynthesize ZnO NPs utilizing endophyte Trichoderma viride, isolated from the seeds of Momordica charantia. The physicochem. characterization of NPs was done via employing a combination of spectroscopic and microscopic techniques. The NPs were found to have a hexagonal shape and possessed an average particle size of around 63.3 nm. The antimicrobial activity of NPs was evaluated against multi-drug resistant organisms and it was observed to be an appreciable one whereas the antioxidant activity was deduced to be dose-dependent. Thus, these ZnO NPs can be considered as a probable active ingredient of any future therapeutic conceptualization after undertaking a thorough toxicol. assessment. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7COA of Formula: C16H18FN3O3).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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. 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. COA of Formula: C16H18FN3O3

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

Leus, Inga V. et al. published their research in Scientific Reports in 2022 | CAS: 70458-96-7

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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. Category: piperazines

Property space mapping of Pseudomonas aeruginosa permeability to small molecules was written by Leus, Inga V.;Weeks, Jon W.;Bonifay, Vincent;Shen, Yue;Yang, Liang;Cooper, Connor J.;Nash, Dinesh;Duerfeldt, Adam S.;Smith, Jeremy C.;Parks, Jerry M.;Rybenkov, Valentin V.;Zgurskaya, Helen I.. And the article was included in Scientific Reports in 2022.Category: piperazines The following contents are mentioned in the article:

Two membrane cell envelopes act as selective permeability barriers in Gram-neg. bacteria, protecting cells against antibiotics and other small mols. Significant efforts are being directed toward understanding how small mols. permeate these barriers. In this study, we developed an approach to analyze the permeation of compounds into Gram-neg. bacteria and applied it to Pseudomonas aeruginosa, an important human pathogen notorious for resistance to multiple antibiotics. The approach uses mass spectrometric measurements of accumulation of a library of structurally diverse compounds in four isogenic strains of P. aeruginosa with varied permeability barriers. We further developed a machine learning algorithm that generates a deterministic classification model with minimal synonymity between the descriptors. This model predicted good permeators into P. aeruginosa with an accuracy of 89% and precision above 58%. The good permeators are broadly distributed in the property space and can be mapped to six distinct regions representing diverse chem. scaffolds. We posit that this approach can be used for more detailed mapping of the property space and for rational design of compounds with high Gram-neg. permeability. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Category: piperazines).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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. Category: piperazines

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

Niewiadomy, Andrzej’s team published research in Acta Poloniae Pharmaceutica in 72 | CAS: 87179-40-6

Acta Poloniae Pharmaceutica published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Name: (E)-1-Cinnamylpiperazine.

Niewiadomy, Andrzej published the artcileSynthesis and biological activity of novel N,n-cyclic-2,4-dihydroxythiobenzamide derivatives, Name: (E)-1-Cinnamylpiperazine, the publication is Acta Poloniae Pharmaceutica (2015), 72(5), 943-950, database is CAplus.

A series of novel N,N-cyclic-2,4-dihydroxythiobenzamide derivatives is described. Test compounds were formed by the reaction of the com. available reagents with sulfinylbis[(2,4- dihydroxyphenyl)methanethione] (STB). The chem. structures were confirmed by IR, 1H NMR, 13CNMR, EI-MS, and elemental anal. For the estimation of potential activity in vitro, the MIC values against strains of Candida were determined Antifungal properties of selected compounds under in vitro conditions against five phytopathogenic fungi were estimated Furthermore, the antiproliferative activity against the HCV29T cancer cell lines has been studied. These compounds exhibited antiproliferative activity in the range of 33.98 n 10.51 μg/mL.

Acta Poloniae Pharmaceutica published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Name: (E)-1-Cinnamylpiperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Chen, Yan’s team published research in ACS Medicinal Chemistry Letters in 13 | CAS: 55403-35-5

ACS Medicinal Chemistry Letters published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C10H16N4, Category: piperazines.

Chen, Yan published the artcileDiscovery of 5-Aryl-2,4-diaminopyrimidine Compounds as Potent and Selective IRAK4 Inhibitors, Category: piperazines, the publication is ACS Medicinal Chemistry Letters (2022), 13(4), 714-719, database is CAplus and MEDLINE.

IRAK4 kinase plays a key role in TLR/IL-1R signaling pathways that regulate innate immune responses, and if uncontrolled, it is responsible for various inflammatory disorders. By high-throughput screening (HTS) and hit-to-lead optimization, compounds with a 5-aryl-2,4-diaminopyrimidine core structure have been identified as potent IRAK4 inhibitors. A cocrystal structure of IRAK4 protein with an early lead mol. helped with understanding the structure-activity relationship and the design of the new compounds Initial HTS hits from this series of compounds were also found to inhibit TAK1 kinase, which would cause liver toxicity and potentially bone marrow failure. Optimization of this series resulted in improved selectivity over TAK1 kinase. The TAK1 selectivity was found to be closely associated with different sizes and types of substituents at the 5-position of the pyrimidine. The impact of other pyrimidine substituents on the potency and selectivity was also explored. A few representative compounds were evaluated in IL-1β-induced IL-6 inhibition animal model studies and showed modest efficacy.

ACS Medicinal Chemistry Letters published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C10H16N4, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Yadav, Mangal S.’s team published research in ACS Omega in 4 | CAS: 87179-40-6

ACS Omega published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C26H41N5O7S, Application of (E)-1-Cinnamylpiperazine.

Yadav, Mangal S. published the artcileSilicon Industry Waste Polymethylhydrosiloxane-Mediated Benzotriazole Ring Cleavage: A Practical and Green Synthesis of Diverse Benzothiazoles, Application of (E)-1-Cinnamylpiperazine, the publication is ACS Omega (2019), 4(4), 6681-6689, database is CAplus and MEDLINE.

A green modification has been introduced to the synthesis of benzothiazoles by using polymethylhydrosiloxane (PMHS) for successive steps of benzotriazole ring cleavage (BtRC) and cyclization; an approach which was previously developed in our lab by use of n-Bu3SnH. The use of silicone industry byproduct PMHS makes this protocol cost-effective and non-toxic one and thus may be considered for the industrial importance.

ACS Omega published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C26H41N5O7S, Application of (E)-1-Cinnamylpiperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Malinka, W.’s team published research in Pharmazie in 55 | CAS: 87179-40-6

Pharmazie published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Related Products of piperazines.

Malinka, W. published the artcileSynthesis of some N-substituted 3,4-pyrroledicarboximides as potential CNS depressive agents, Related Products of piperazines, the publication is Pharmazie (2000), 55(1), 9-16, database is CAplus and MEDLINE.

Several novel N-substituted 3,4-pyrroledicarboximides were prepared and eleven representatives were examined in a series of in vivo CNS tests. A few of these compounds displayed a similar profile of biol. selectivity to that of 3,4-pyrroledicarboximides described previously; their structure-activity relationships are discussed.

Pharmazie published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Related Products of piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Malinka, W.’s team published research in Pharmazie in 55 | CAS: 87179-40-6

Pharmazie published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Application In Synthesis of 87179-40-6.

Malinka, W. published the artcileSynthesis and preliminary screening of derivatives of 2-(4-arylpiperazin- 1-ylalkyl)-3-oxoisothiazolo[5,4-b]pyridines as CNS and antimycobacterial agents, Application In Synthesis of 87179-40-6, the publication is Pharmazie (2000), 55(6), 416-425, database is CAplus and MEDLINE.

Isothiazolopyridines, e.g. I (X = S, SO2; X1 = CO, CH2CH2, CH2CH2CH2; R = H, 3-Cl, 3-CF3, 2-MeO), were prepared that possess a side chain at the isothiazole ring typical, among others, for trazodone or NAN-195. Representatives of these novel isothiazolopyridines were examined for acute toxicity and in several commonly used CNS tests in mice and for arterial blood pressure in rats. Three of the five compounds tested showed significant analgesic activity. The most active compound, I (X = S; X1 = CH2CH2; R = 3-Cl) exhibited analgesic action in the writhing test in a dose 1/1280 of LD50 (LD50 = 1135.5 mg/kg) after administration i.p. to mice. Addnl., the compounds described here and related isothiazolopyridines obtained previously were evaluated against Mycobacterium tuberculosis H37Rv at 12.5 μg/mL in in vitro assays. Seven of the nineteen compounds tested showed 100% inhibition of that mycobacterium.

Pharmazie published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Application In Synthesis of 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics