Category: 109-01-3

Category: piperazinesIn 2022 ,《Design and synthesis of novel quinazolinone derivatives as anti-HBV agents with TLR8 agonist effect》 appeared in European Journal of Medicinal Chemistry. The author of the article were Qiu, Jingying; Zhou, Qingqing; Zou, Yueting; Li, Shuqiong; Yang, Lihua; Chen, Wang; Gao, Jian; Gu, Xiaoke. The article conveys some information:

In this work, a series of novel quinazolinone derivatives I [R1 = benzyl, 2-furylmethyl, 2-thienylmethyl, etc.; R2 = H, 2-MeO, 3-F, etc.; R3 = (4-methylpiperazin-1-yl), (4-hydroxy-1-piperidyl), (2-aminopyrimidin-4-yl)oxy, etc.] were synthesized and evaluated as novel anti-HBV agents. Among them, compound I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] exhibited potent inhibitory effect on HBV DNA replication in both wild type and drug resistant (lamivudine and entecavir) HBV strains with IC50 values of 0.15 and 0.10μM, resp. Notably, the selective index value of I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] was high above 66.67, indicating the favorable safety profile. Mol. docking study indicated that compound I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] well fitted into the binding pocket of TLR8 protein-protein interface. Dual-luciferase reporter gene assay further confirmed that compound I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] could dose-dependently activate TLR8, thus effectively inducing the activity of TLR8-dependent NF-κB. Collectively, compound I [R1 = 2-furylmethyl; R2 = 2-MeO; R3 = (2-aminopyrimidin-4-yl)oxy] displayed potent anti-HBV activities and TLR8 agonist effect in vitro, and might be a potential immunomodulatory anti-HBV agent to warrant further investigation. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Category: piperazines)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Category: piperazines

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

HPLC of Formula: 109-01-3In 2022 ,《Structural and PK-guided identification of indole-based non-acidic autotaxin (ATX) inhibitors exhibiting high in vivo anti-fibrosis efficacy in rodent model》 was published in European Journal of Medicinal Chemistry. The article was written by Lei, Hongrui; Cao, Zhi; Wu, Huinan; Li, Tong; Wang, Xinyu; Chen, Yuxiang; Ma, Enlong; Sun, Lixin; Zhai, Xin. The article contains the following contents:

In recent decades, pharmacol. targeting of the autotaxin (ATX)/lysophosphatidic acid (LPA) axis accounted for excellent disease management benefits. Herein, to extend the scope of structure-activity relationships (SARs), fifteen indole-based carbamate derivatives I [R = 4-Me, 3,4-difluoro, 2,3-dichloro; R1 = pyrrolidin-1-yl, (4-methyl-1-piperidyl), (4-methylpiperazin-1-yl); R2 = H, CH3, etc] were prepared to evaluate the ATX inhibitory potency. Among them, compound I [R = 3,5-dichloro; R1 = morpholino; R2 = H] bearing morpholine moiety was identified as the optimal ATX inhibitor (0.41 nM), superior to the pos. control GLPG1690 (2.90 nM). To resolve the intractable issue of poor pharmacokinetic (PK) property, urea moiety was introduced as a surrogate of carbamate which furnished compounds II [R3 = morpholino, (4-hydroxy-1-piperidyl), [2-(hydroxymethyl)pyrrolidin-1-yl]; R4 = H, 4-Cl, 4-F, etc]. The dedicated modification identified the diethanolamine entity II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)] with satisfactory water solubility and PK profiles with a min. sacrifice of ATX inhibition (2.17 nM). The most promising candidate II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)] was evaluated for anti-fibrosis effect in a bleomycin challenged mice lung fibrosis model. Upon treatment with II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)], the in vivo ATX activity in both lung homogenate and broncheoalveolar fluid (BALF) sample was significantly down-regulated. Furthermore, the gene expression of pro-fibrotic cytokines transforming growth factor-β (TGF-β), interleukin- 6 (IL-6) and tumor necrosis factor-α (TNF-α) in lung tissue was reduced to normal level. Collectively, the promising biol. effects may advocate potential application of II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)] in fibrosis relevant diseases. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..HPLC of Formula: 109-01-3

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

《Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Rani, Sudesh; Paul, Kamaldeep. SDS of cas: 109-01-3 The article mentions the following:

To structurally relate anticancer drug tamoxifen used in the treatment of breast cancer, a sequence of compounds I [R = piperidinyl, morpholino, 4-methylpiperazinyl, 4-ethylpiperazinyl, etc.] were designed and synthesized as potential drug candidates. McMurry coupling reaction was used as the key synthetic step in the preparation of these compounds I and the ratios of E/Z-isomers were determined on the basis of NMR and HPLC experiments The new compounds I were found to be cytotoxic in the micromolar range with 60 human tumor cell lines at one dose and five dose concentration levels. Detailed studies on the most active compounds I [R = 2-morpholinoethyl amine, cyclohexylamine and diethylamine] show these compounds were capable to inhibit the growth of cancer cells. Finally, with the aim to correlate the antiproliferative activity with an intracellular target(s), the effect on relaxation activity of DNA topoisomerase-II was assayed. The relevance of interaction of most active compounds with topoisomerase-II was demonstrated which was also supported by docking studies. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3SDS of cas: 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..SDS of cas: 109-01-3

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

The author of 《Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties》 were Lei, Hongrui; Jiang, Nan; Miao, Xiuqi; Xing, Lingyun; Guo, Ming; Liu, Yang; Xu, Haowen; Gong, Ping; Zuo, Daiying; Zhai, Xin. And the article was published in European Journal of Medicinal Chemistry in 2019. Reference of 1-Methylpiperazine The author mentioned the following in the article:

Aiming to identify novel potent ALK and ROS1 dual inhibitors, the relatively bulky piperidine fragment in ceritinib was replaced with substituted imidazolidin-2-one moiety which gave rise to a series of 2,4-diaryl-aminopyrimidine (DAAP) analogs. SAR studies were conducted based on cellular assays on five cell lines and most compounds exerted moderated to excellent activities. Among them, 15(I) showed excellent inhibitory activities against ROS1 and ALK pos. cell lines, especially Ba/F3G1202R, with IC50 values ranging from 14 to 37 nM. As a continuation, several compounds were tested in enzymic assays and I displayed encouraging activities against wild-type ALK (1.2 nM), ROS1(0.43 nM) as well as extremely resistant ALKL1196M and ALKG1202R mutants with IC50 values of 0.73 nM and 6.7 nM, resp. To our delight, both cellular and enzymic results of I were in good accordance with western blot assays on H2228 and HCC78 cell lines. Importantly, pharmacokinetic (PK) profiles of I were obtained with quite satisfying AUC and Cmax values. Besides, the binding models of I with ALKWT, ALKG1202R and ROS1 clearly present the essential interactions within the active site. The experimental part of the paper was very detailed, including the reaction process of 1-Methylpiperazine(cas: 109-01-3Reference of 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Reference of 1-Methylpiperazine

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

Recommanded Product: 1-MethylpiperazineIn 2019 ,《Sulfonamide Synthesis through Electrochemical Oxidative Coupling of Amines and Thiols》 was published in Journal of the American Chemical Society. The article was written by Laudadio, Gabriele; Barmpoutsis, Efstathios; Schotten, Christiane; Struik, Lisa; Govaerts, Sebastian; Browne, Duncan L.; Noel, Timothy. The article contains the following contents:

Sulfonamides are key motifs in pharmaceuticals and agrochems., spurring the continuous development of novel and efficient synthetic methods to access these functional groups. Herein, the authors report an environmentally benign electrochem. method which enables the oxidative coupling between thiols and amines, two readily available and inexpensive commodity chems. The transformation is completely driven by electricity, does not require any sacrificial reagent or addnl. catalysts and can be carried out in only 5 min. Hydrogen is formed as a benign byproduct at the counter electrode. Owing to the mild reaction conditions, the reaction displays a broad substrate scope and functional group compatibility. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 1-Methylpiperazine

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

The author of 《Synthesis and antifungal activity of 1-aminomethyl-3-[4′-(4”-fluorobenzyloxy)-benzohydrazono] isatins》 were Rastogi, Nisheeth. And the article was published in Indian Journal of Heterocyclic Chemistry in 2019. Reference of 1-Methylpiperazine The author mentioned the following in the article:

A new series of 1-aminomethyl-3-[4′-(4”-fluorobenzyloxy)benzohydrazono]isatins (Mannich bases) I [R = H, Me, morpholinomethyl, etc.] were synthesized and screened for their antifungal potential against human pathogenic fungi. The structures of the compounds were established by means of elemental anal. and spectral data (IR and 1H NMR). The experimental part of the paper was very detailed, including the reaction process of 1-Methylpiperazine(cas: 109-01-3Reference of 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Reference of 1-Methylpiperazine

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

Recommanded Product: 1-MethylpiperazineIn 2021 ,《Facile and Cost-Effective Route for the Synthesis of Simmerafil》 was published in Organic Process Research & Development. The article was written by Odilov, Abdullajon; Liu, Yin; Hu, Tianwen; Jiang, Xiangrui; Suo, Jin; Tian, Guanghui; Yang, Feipu; Shen, Jingshan. The article contains the following contents:

An improved synthesis of simmerafil, a potent PDE5 inhibitor as a clin. candidate, is described with a 38.1% overall yield and 99.7% purity. Starting from the safe and inexpensive salicylamide, the key intermediate 2-propoxybenzimidamide, which is also a potential precursor for the preparation of pyrimidinone derivatives, was effectively and conveniently obtained. The subsequent process from 2-propoxybenzimidamide to simmerafil was optimized, which makes it more amenable to scale-up.1-Methylpiperazine(cas: 109-01-3Recommanded Product: 1-Methylpiperazine) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 1-Methylpiperazine

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

Related Products of 109-01-3In 2021 ,《Discovery and optimization of novel pyrazole-benzimidazole CPL304110 as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3)》 appeared in European Journal of Medicinal Chemistry. The author of the article were Yamani, Abdellah; Zdzalik-Bielecka, Daria; Lipner, Joanna; Stanczak, Aleksandra; Piorkowska, Natalia; Stanczak, Paulina Seweryna; Olejkowska, Patrycja; Hucz-Kalitowska, Joanna; Magdycz, Marta; Dzwonek, Karolina; Dubiel, Krzysztof; Lamparska-Przybysz, Monika; Popiel, Delfina; Pieczykolan, Jerzy; Wieczorek, Maciej. The article conveys some information:

The scaffolds hybridization approach, scaffold-hopping concept, has been employed to synthesize a series of novel pyrazole-benzimidazoles I [R1 = H, Cl; R2 = morpholin-4-yl, 4-methylpiperazin-1-ylcarbonyl, tetrahydropyran-4-ylcarbamoyl, etc.; R3 = H, F]. Compound I [R1 = R3 = H; R2 = 4-methylpiperazin-1-yl] (CPL304110) was identified as a selective and potent pan-FGFR inhibitor for FGFR1, FGFR2, FGFR3 with IC50 of 0.75 nM, 0.50 nM, 3.05 nM resp., and IC50 of 87.90 nM for FGFR4. Due to its favorable pharmacokinetic profile, low toxicity and potent anti-tumor activity in-vivo, this compound I is currently under evaluation in phase I clin. trial for the treatment of bladder, gastric and squamous cell lung cancers (01FGFR2018; NCT04149691). In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Related Products of 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Related Products of 109-01-3

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

《Synthesis, biological evaluation and molecular docking studies of some new 2-(2-(substituted piperazin-1-yl)-phenyl)-1H-benzo[d]imidazoles as potential antibacterial, anticancer and antifungal agents》 was written by Bhardwaj, Harsh; Sharma, C. S.. Related Products of 109-01-3 And the article was included in Indian Journal of Heterocyclic Chemistry in 2020. The article conveys some information:

Some new 2-(2-(substituted piperazin-1-yl)-phenyl)-1H-benzo[d]imidazoles I [R = H, 2-Me, 4-Et, etc.] were designed, synthesized and evaluated by the docking studies using glide tool for their antimicrobial and anticancer activities. The structures of these compounds I were characterized by IR, proton NMR, mass spectral data, and elemental anal. Each analog was tested in-vitro for various types of pharmacol. activities, including antibacterial, antifungal and anticancer activity. The compound I [R = 3-Me] was found to be most active against Escherichia coli and Pseudomonas aeruginosa and compound I [R = 2-Et] against Bacillus subtilis and Staphylococcus aureus. The derivative I [R = 4-Et] showed good activity against Candida albicans and Aspergillus niger. Among all the tested compounds, I [R = H, 2-Me] were found with significant anticancer activity in comparison to Adriamycin standard drug. The obtained results revealed that most of the synthesized compounds I exhibited significant antifungal, antibacterial and anticancer activity. It was deduced that these synthesized compounds I can be regarded as a promising starting point for developing a single mol. with multiple targets.1-Methylpiperazine(cas: 109-01-3Related Products of 109-01-3) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Related Products of 109-01-3

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

Computed Properties of C5H12N2In 2020 ,《The effect of novel 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b] [1,2,4]triazine sulfonamide derivatives on apoptosis and autophagy in DLD-1 and HT-29 colon cancer cells》 appeared in International Journal of Molecular Sciences. The author of the article were Gornowicz, Agnieszka; Szymanowska, Anna; Mojzych, Mariusz; Bielawski, Krzysztof; Bielawska, Anna. The article conveys some information:

The objective of this study was to synthesize title compounds I (R = [(2S)-1-hydroxy-4-methylpentan-2-yl]aminyl, 4-methylpiperazin-1-yl) by utilizing nucleophilic substitution reaction at the position N1. The biol. activity of tested compounds was assessed in DLD-1 and HT-29 cell lines. The induction of apoptosis was confirmed by Annexin V binding assay and acridine orange/ethidium bromide staining. The loss of mitochondrial membrane potential and caspase-8 activity was estimated using cytometer flow anal. The concentration of p53, LC3A, LC3B and beclin-1 was measured using the ELISA technique. The study revealed that anticancer activity of title compounds I is related with initiation of apoptosis occurred on the intrinsic pathway with mitochondrial membrane decrease and extrinsic with increase of activity of caspase-8. Moreover, a decrease in beclin-1, LC3A, and LC3B was observed in two cell lines after treatment with novel compounds This study showed that novel title compounds I might be a potential strategy in colon cancer treatment. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Computed Properties of C5H12N2)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Computed Properties of C5H12N2

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