Meyer, Walter E.’s team published research in Journal of Medicinal Chemistry in 32 | CAS: 71260-16-7

Journal of Medicinal Chemistry published new progress about 71260-16-7. 71260-16-7 belongs to piperazines, auxiliary class Piperazine, name is 2-Methyl-1-(piperazin-1-yl)propan-1-one, and the molecular formula is C8H16N2O, Computed Properties of 71260-16-7.

Meyer, Walter E. published the artcile5-(1-Piperazinyl)-1H-1,2,4-triazol-3-amines as antihypertensive agents, Computed Properties of 71260-16-7, the publication is Journal of Medicinal Chemistry (1989), 32(3), 593-7, database is CAplus and MEDLINE.

A series of 5-(1-piperazinyl)-1H-1,2,4-triazol-3-amines was synthesized and screened for antihypertensive and diuretic activity in spontaneously hypertensive rats (SHR). One compound, 5-[4-[(3-chlorophenyl)methyl]-1-piperazinyl]-1H-1,2,4-triazol-3-amine (I), was selected to define the mechanism of its antihypertensive activity. Studies in spontaneously hypertensive rats suggest ganglionic blocking activity. Short-lived antihypertensive activity was observed in conscious renal hypertensive dogs. Structure-activity relationships are discussed. None of the prepared and tested compounds had diuretic activity.

Journal of Medicinal Chemistry published new progress about 71260-16-7. 71260-16-7 belongs to piperazines, auxiliary class Piperazine, name is 2-Methyl-1-(piperazin-1-yl)propan-1-one, and the molecular formula is C8H16N2O, Computed Properties of 71260-16-7.

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

Prabhakaran, Jaya’s team published research in Bioorganic & Medicinal Chemistry Letters in 20 | CAS: 87179-40-6

Bioorganic & Medicinal Chemistry Letters 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.

Prabhakaran, Jaya published the artcileSynthesis and in vivo evaluation of [11C]MPTQ: A potential PET tracer for alpha2A-adrenergic receptors, Name: (E)-1-Cinnamylpiperazine, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(12), 3654-3657, database is CAplus and MEDLINE.

Radiosynthesis and in vivo evaluation of [N-methyl-11C] 5-methyl-3-[4-(3-phenylallyl)-piperazin-1-ylmethyl]-3,3a,4,5-tetrahydroisoxazolo[4,3-c]quinoline, I (R = 11CH3)(II), a potential PET tracer for alpha2-adrenergic receptors is described. Syntheses of nonradioactive standard and corresponding desmethyl precursor I (R = Me, H) were achieved from 2-aminobenzaldehyde in 40% and 65% yields, resp. Methylation using [11C]CH3I in the presence of aqueous potassium hydroxide in DMSO afforded II in 25% yield (EOS, end of synthesis) with >99% chem. and radiochem. purities with a specific activity range from 3-4 Ci/¦Ìmol (n = 6). The total synthesis time was 30 min from EOB (end of bombardment). PET (Positron-emission tomog.) studies in anesthetized baboon show that II penetrates the BBB (blood brain barrier) and accumulates in alpha2A-AR enriched brain areas.

Bioorganic & Medicinal Chemistry Letters 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

Temps, Carolin et al. published their research in Cancer Research in 2021 |CAS: 380843-75-4

The Article related to breast cancer src conformation lymphocyte ecf506 antiproliferative, Placeholder for records without volume info and other aspects.Application of 380843-75-4

On November 1, 2021, Temps, Carolin; Lietha, Daniel; Webb, Emily R.; Li, Xue-Feng; Dawson, John C.; Muir, Morwenna; Macleod, Kenneth G.; Valero, Teresa; Munro, Alison F.; Contreras-Montoya, Rafael; Luque-Ortega, Juan R.; Fraser, Craig; Beetham, Henry; Schoenherr, Christina; Lopalco, Maria; Arends, Mark J.; Frame, Margaret C.; Qian, Bin-Zhi; Brunton, Valerie G.; Carragher, Neil O.; Unciti-Broceta, Asier published an article.Application of 380843-75-4 The title of the article was A conformation selective mode of inhibiting SRC improves drug efficacy and tolerability. And the article contained the following:

Despite the approval of several multikinase inhibitors that target SRC and the overwhelming evidence of the role of SRC in the progression and resistance mechanisms of many solid malignancies, inhibition of its kinase activity has thus far failed to improve patient outcomes. Here we report the small mol. eCF506 locks SRC in its native inactive conformation, thereby inhibiting both enzymic and scaffolding functions that prevent phosphorylation and complex formation with its partner FAK. This mechanism of action resulted in highly potent and selective pathway inhibition in culture and in vivo. Treatment with eCF506 resulted in increased antitumor efficacy and tolerability in syngeneic murine cancer models, demonstrating significant therapeutic advantages over existing SRC/ABL inhibitors. Therefore, this mode of inhibiting SRC could lead to improved treatment of SRC-associated disorders. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Application of 380843-75-4

The Article related to breast cancer src conformation lymphocyte ecf506 antiproliferative, Placeholder for records without volume info and other aspects.Application of 380843-75-4

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

Fan, Mengtian et al. published their research in Journal of Cellular and Molecular Medicine in 2021 |CAS: 380843-75-4

The Article related to lung cancer cx3cl1 tyrosine phosphorylation, cx3cl1, cancer, cortactin, invasion, lung, Mammalian Pathological Biochemistry: Oncology and other aspects.SDS of cas: 380843-75-4

Fan, Mengtian; Wu, Jinghong; Li, Xian; Jiang, Yingjiu; Wang, Xiaowen; Bie, Mengjun; Weng, Yaguang; Chen, Sicheng; Chen, Bin; An, Liqin; Zhang, Menghao; Huang, Gaigai; Zhu, Mengying; Shi, Qiong published an article in 2021, the title of the article was CX3CL1 promotes tumour cell by inducing tyrosine phosphorylation of cortactin in lung cancer.SDS of cas: 380843-75-4 And the article contains the following content:

It has been reported that chemokine CX3CL1 can regulate various tumors by binding to its unique receptor CX3CR1. However, the effect of CX3CL1-CX3CR1 on the lung adenocarcinoma and lung squamous cell carcinoma is still unclear. Here, we showed that CX3CL1 can further invasion and migration of lung adenocarcinoma A549 and lung squamous cell carcinoma H520. In addition, Western blot and immunofluorescence test indicated CX3CL1 up-regulated the phosphorylation level of cortactin, which is a marker of cell pseudopodium. Meanwhile, the phosphorylation levels of c-Src and c-Abl, which are closely related to the regulation of cortactin phosphorylation, are elevated. Nevertheless, the src/abl inhibitor bosutinib and mutations of cortactin phosphorylation site could inhibit the promotion effect of CX3CL1 on invasion and migration of A549 and H520. Moreover, these results of MTT, Hoechst staining and Western blot suggested that CX3CL1 had no effect on the proliferation and apoptosis of A549 and H520 in vitro. The effects of CX3CL1 were also verified by the s.c. tumor formation in nude mice, which showed that it could promote proliferation and invasion of A549 in vivo. In summary, our results indicated that CX3CL1 furthered invasion and migration in lung cancer cells partly via activating cortactin, and CX3CL1 may be a potential mol. in regulating the migration and invasion of lung cancer. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).SDS of cas: 380843-75-4

The Article related to lung cancer cx3cl1 tyrosine phosphorylation, cx3cl1, cancer, cortactin, invasion, lung, Mammalian Pathological Biochemistry: Oncology and other aspects.SDS of cas: 380843-75-4

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

Crew, Andrew P. et al. published their patent in 2020 |CAS: 1211568-27-2

The Article related to bifunctional heterocycle preparation raf modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1211568-27-2

On April 30, 2020, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Crews, Craig M.; Jaime-Figueroa, Saul; Dong, Hanqing; Qian, Yimin; Zimmermann, Kurt published a patent.Related Products of 1211568-27-2 The title of the patent was Bifunctional heterocycles, their use in targeted degradation of rapidly accelerated fibrosarcoma polypeptides and their preparation. And the patent contained the following:

The present disclosure relates bifunctional compounds of formula ULM-L-PTM, their use in modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein) and treatment of diseases that result from aggregation or accumulation of the target protein. and their preparation Compounds of formula ULM-L-PTM, wherein ULM is a small mol. E3 ubiquitin ligase binding moiety; PTM is a small mol. comprising a RAF protein targeting moiety; L is a bond or chem. linking moiety connecting ULM and PTM; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorph and prodrug thereof, are claimed. Compound I was prepared using a multistep procedure (procedure given). The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein (data given). The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Related Products of 1211568-27-2

The Article related to bifunctional heterocycle preparation raf modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1211568-27-2

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

Akbar, Abdullah’s team published research in Journal of Medicinal Chemistry in 2017 | CAS: 534615-34-4

1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Recommanded Product: 1-(Isopropylsulfonyl)piperazine

Recommanded Product: 1-(Isopropylsulfonyl)piperazineOn September 28, 2017 ,《Structure-Activity Relationships of Potent, Targeted Covalent Inhibitors That Abolish Both the Transamidation and GTP Binding Activities of Human Tissue Transglutaminase》 was published in Journal of Medicinal Chemistry. The article was written by Akbar, Abdullah; McNeil, Nicole M. R.; Albert, Marie R.; Ta, Viviane; Adhikary, Gautam; Bourgeois, Karine; Eckert, Richard L.; Keillor, Jeffrey W.. The article contains the following contents:

Human tissue transglutaminase (hTG2) is a multifunctional enzyme. It is primarily known for its calcium-dependent transamidation activity that leads to formation of an isopeptide bond between glutamine and lysine residues found on the surface of proteins, but it is also a GTP binding protein. Overexpression and unregulated hTG2 activity have been associated with numerous human diseases, including cancer stem cell survival and metastatic phenotype. Herein, the authors present a series of targeted covalent inhibitors (TCIs) based on the previously reported Cbz-Lys scaffold. From this structure-activity relationship (SAR) study, novel irreversible inhibitors were identified that block the transamidation activity of hTG2 and allosterically abolish its GTP binding ability with a high degree of selectivity and efficiency (kinact/KI > 105 M-1 min-1). One optimized inhibitor (VA4) was also shown to inhibit epidermal cancer stem cell invasion with an EC50 of 3.9 μM, representing a significant improvement over the previously reported “”hit”” NC9. After reading the article, we found that the author used 1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4Recommanded Product: 1-(Isopropylsulfonyl)piperazine)

1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Recommanded Product: 1-(Isopropylsulfonyl)piperazine

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

1 Sep 2021 News Analyzing the synthesis route of 1-Methylpiperazin-2-one hydrochloride

109384-27-2, The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

(rac)-6-chloro-3-(1 -(4,6-difluoro-1 -isopropyl-1 H-indazol-5-yl)ethyl)imidazo[1 ,2-b]pyridazine (Intermediate U, 56.4 mg, 0.15 mmol), KF (43.6 mg, 0.75 mmol) and 1-methylperazine-2- one hydrochloride (51.4 mg, 0.45 mmol) were suspended in NMP (0.4 ml_). The RM was stirred at 180 0C for 4 h. The mixture was diluted with EtOAc and washed with NaHCO3 10% (2 x) and water (4 x). The combined organic layers were dried over Na2SO4, filtered and concentrated. The residue was purified by flash chromatography and afforded the title compound as a light brown foam (tR 4.06 min (conditions 5), MH+ = 454.3, 1H-NMR in DMS0-d6: 8.09 (s, 1 H); 7.81 (d, 1 H); 7.53 (s, 1 H); 7.43 (d, 1H); 7.05 (d, 1 H), 4.86 (m, 2H); 4.03 (d, 1H); 3.81 (d, 1H); 3.64 (m, 2H); 3.24 (m, 2H); 2.80 (s, 3H); 1.79 (d, 3H), 1.41 (m, 6H)).

109384-27-2, The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NOVARTIS AG; FURET, Pascal; McCARTHY, Clive; SCHOEPFER, Joseph; STUTZ, Stefan; WO2011/15652; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics