Tag: 100-200

Reference of 2-(Piperidin-4-yl)ethanolIn 2020 ,《Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent》 was published in Journal of Medicinal Chemistry. The article was written by Kurasawa, Osamu; Miyazaki, Tohru; Homma, Misaki; Oguro, Yuya; Imada, Takashi; Uchiyama, Noriko; Iwai, Kenichi; Yamamoto, Yukiko; Ohori, Momoko; Hara, Hideto; Sugimoto, Hiroshi; Iwata, Kentaro; Skene, Robert; Hoffman, Isaac; Ohashi, Akihiro; Nomura, Toshiyuki; Cho, Nobuo. The article contains the following contents:

In our pursuit of developing a novel, potent, and selective cell division cycle 7 (Cdc7) inhibitor, we optimized the previously reported thieno[3,2-d]pyrimidinone analog I showing time-dependent Cdc7 kinase inhibition and slow dissociation kinetics. These medicinal chem. efforts led to the identification of compound 3d, which exhibited potent cellular activity, excellent kinase selectivity, and antitumor efficacy in a COLO205 xenograft mouse model. However, the issue of formaldehyde adduct formation emerged during a detailed study of 3d, which was deemed an obstacle to further development. A structure-based approach to circumvent the adduct formation culminated in the discovery of compound 11b (TAK-931) possessing a quinuclidine moiety as a preclin. candidate. In this paper, the design, synthesis, and biol. evaluation of this series of compounds will be presented. In the experiment, the researchers used many compounds, for example, 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Reference of 2-(Piperidin-4-yl)ethanol)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKReference of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhou, Yu; Li, Xiaoguang; Chen, Kerong; Ba, Qian; Zhang, Xu; Li, Jingquan; Wang, Jinfang; Wang, Hui; Liu, Hong published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Structural optimization and biological evaluation for novel artemisinin derivatives against liver and ovarian cancers》.Application In Synthesis of 2-(Piperidin-4-yl)ethanol The article contains the following contents:

An increasing number of artemisinin (ARS) and its derivatives have been reported for their potential therapeutic value of human cancer. However, their therapeutic potencies are limited owing to their poor pharmacokinetic profiles. Our previous studies showed that lead compound I originated from incorporating the pharmacophore of the approved chemotherapeutic agent melphalan into the basic skeleton of artemisinin with a succinic linker exhibited an excellent toxicity to human ovarian cancer cells and low cytotoxicity to normal cells. The mechanism studies demonstrated that it inhibited the growth and proliferation of ovarian cancer cells and resulted in S-phase arrest, apoptosis and inhibition of migration. Meanwhile, it exhibited excellent antitumor activities in animal models. Herein, further structure optimization for this lead compound I was performed and nineteen novel derivatives were designed and synthesized. Several compounds demonstrated powerful cytotoxic effects against human liver cancer and ovarian cancer cell lines, with their IC50s below 0.86μM against Hep3B and A2780 cell lines, which are superior to that of I. Four compounds were selected to further evaluate their antitumor activities in in vitro and in vivo ovarian and liver cancer models; the results indicated that compound II exhibited the best therapeutic effect, not only effectively inhibiting the growth of 7404 xenograft and Huh7 xenograft, but also presenting a good dose-dependent inhibition toward the growth of A2780 xenograft. Overall, based on these pos. results, these novel chem. structures may provide a new inspiration for the discovery of novel antitumor agents originated from artemisinin scaffolds.2-(Piperidin-4-yl)ethanol(cas: 622-26-4Application In Synthesis of 2-(Piperidin-4-yl)ethanol) was used in this study.

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Application In Synthesis of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《A Buchwald-Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3-Ligase PROTACs**》 was written by Hayhow, Thomas G.; Borrows, Rachel E. A.; Diene, Coura R.; Fairley, Gary; Fallan, Charlene; Fillery, Shaun M.; Scott, James S.; Watson, David W.. Product Details of 622-26-4 And the article was included in Chemistry – A European Journal in 2020. The article conveys some information:

A palladium-catalyzed Buchwald-Hartwig amination for lenalidomide-derived aryl bromides was optimized using high throughput experimentation (HTE) to afford isoindolyl amines I [R1 = H, Me; R2 = n-Bu, Ph, 2-MeC6H4, etc.; R1R2 = (CH2)2O(CH2)2, (CH2)2CH(CH2OH)(CH2)2, (CH2)2N(Boc)(CH2)2, etc.]. The substrate scope of the optimized conditions was evaluated for a range of alkyl- and aryl- amines and functionalised aryl bromides. The methodol. allowed access to new cereblon-based bifunctional proteolysis targeting chimeras with a reduced step count and improved yields. The results came from multiple reactions, including the reaction of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Product Details of 622-26-4)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Product Details of 622-26-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2012,Bollinger, Markus; Manzenrieder, Florian; Kolb, Roman; Bochen, Alexander; Neubauer, Stefanie; Marinelli, Luciana; Limongelli, Vittorio; Novellino, Ettore; Moessmer, Georg; Pell, Reinhard; Lindner, Wolfgang; Fanous, Joseph; Hoffman, Amnon; Kessler, Horst published 《Tailoring of Integrin Ligands: Probing the Charge Capability of the Metal Ion-Dependent Adhesion Site》.Journal of Medicinal Chemistry published the findings.Recommanded Product: 2-(Piperidin-4-yl)ethanol The information in the text is summarized as follows:

Intervention in integrin-mediated cell adhesion and integrin signaling pathways is an ongoing area of research in medicinal chem. and drug development. One key element in integrin-ligand interaction is the coordination of the bivalent cation at the metal ion-dependent adhesion site (MIDAS) by a carboxylic acid function, a consistent feature of all integrin ligands. With the exception of the recently discovered hydroxamic acids, all bioisosteric attempts to replace the carboxylic acid of integrin ligands failed. We report that phosphinates as well as monomethyl phosphonates represent excellent isosters, when introduced into integrin antagonists for the platelet integrin αIIbβ3. The novel inhibitors exhibit in vitro and ex vivo activities in the low nanomolar range. Steric and charge requirements of the MIDAS region were unraveled, thus paving the way for an in silico prediction of ligand activity and in turn the rational design of the next generation of integrin antagonists. In the experiment, the researchers used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Recommanded Product: 2-(Piperidin-4-yl)ethanol)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Recommanded Product: 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wang, Yi; Ji, Qingjie; Xu, Jixiang; Wan, Jun; Wang, Lei published their research in Separation and Purification Technology on December 1 ,2021. The article was titled 《Activation of peroxydisulfate using N-doped carbon-encapsulated Ni species for efficient degradation of tetracycline》.Quality Control of Triacetonamine The article contains the following contents:

In this study, N-doped porous carbon materials embedded with NiNx species (Ni@NC) were fabricated via the pyrolysis of Ni-doped zeolitic imidazolate frameworks-8 (ZIF-8) at the temperature of 900°C. The obtained Ni@NC-1 catalyst exhibited excellent activity in activating the peroxydisulfate (PDS) that was used for removing tetracycline (TC). The catalytic system exhibited good stability, wide pH adaptation, and high resistance to the operational environment. It was supposed that NiNx species could attach to PDS and act as electron acceptors to receive the electrons for activating the PDS, thus generating highly reactive superoxide radicals (·O-2) and singlet oxygen (1O2) species for rapid degradation of TC. The electron transfer and dissolved oxygen-derived ·O-2 were also responsible for the degradation of TC. In addition, the Ni@NC-1/PDS system exhibited high efficiency for removing oxytetracycline, ciprofloxacin, or levofloxacin. The results of this study would promote the design of other MOFs-derived carbon-encapsulated metal species for efficiently activating persulfate to remove antibiotics from the wastewater. In the experiment, the researchers used Triacetonamine(cas: 826-36-8Quality Control of Triacetonamine)

Triacetonamine(cas: 826-36-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Quality Control of Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Synthesis of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole analogues and their evaluation as anti-Parkinson’s agents》 were Tiwari, Shashi B.; Kohli, D. V.. And the article was published in Medicinal Chemistry Research in 2008. Recommanded Product: 1690-72-8 The author mentioned the following in the article:

A series of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole derivatives, e.g., I, was prepared and their evaluation for anti-Parkinson’s activity was measured in vivo using albino rats. The result of the biol. activity studies indicated that some of the synthesized compounds have good agonistic activity on the dopamine receptors and a few of them were also found to be free from neurotoxicity. Thus these compounds might be useful ligands for studying the functional role of dopamine receptors in vivo. The high log P value of the compounds indicates that they should easily cross the blood-brain barrier (log P > 2.6). In the experimental materials used by the author, we found Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Recommanded Product: 1690-72-8)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Recommanded Product: 1690-72-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Liang, Dongmin; Hu, Yongyou; Xiao, Chun; Wang, Guobin; Xie, Jieyun; Zhu, Xiaoqiang published their research in Science of the Total Environment on August 15 ,2022. The article was titled 《Highly efficient catalytic ozonation for ammonium in water upon γ-Al2O3@Fe/Mg with acidic-basic sites and oxygen vacancies》.Electric Literature of C9H17NO The article contains the following contents:

Catalytic ozonation has prospects in the advanced treatment of nitrogen removal, and solid base MgO can efficiently catalyze the ozonation of ammonium nitrogen. However, it is necessary to improve the problem of easy loss, difficult recovery, and low percentage of gaseous products. Here, MgO, amorphous Fe2O3,and γ-Al2O3 were selected as dopingcomponents and supports, resp., to prepare γ-Al2O3@Fe/Mg composite catalysts with abundant acidic-basicsites and oxygen vacancies. The results show that γ-Al2O3@Fe/Mg5 can efficiently catalyze the ozonation of ammonium nitrogen (98.73%) with 67.82% gaseous product selectivity under the conditions of initial pH = 7, catalyst dosage of 112.88 g/L, and ozone dosage of 2.4 mg/min. The doping of Fe2O3 and MgO with a weaker lattice oxygen binding energy improves the gaseous product selectivity. The mechanism of ammonium nitrogen removal for γ-Al2O3@Fe/Mg5 is revealed, especially the intrinsic contribution of acidic-basic sites and oxygen vacancies. The pH and active sites play different roles in ozone decomposition for NH4+ removal. Surface hydroxyl protonation on basic sites and oxygen vacancies and electron transfer on acidic sites are responsible for ozone decomposition to hydroxyl radicals. Moreover, γ-Al2O3@Fe/Mg5 exhibits good stability, few leaching ions, and can be settled in waterfor easy recovery. This study suggests that γ-Al2O3@Fe/Mg5 is a good candidate for the catalytic ozonation of ammonium nitrogen. After reading the article, we found that the author used Triacetonamine(cas: 826-36-8Electric Literature of C9H17NO)

Triacetonamine(cas: 826-36-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Electric Literature of C9H17NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Reference of TriacetonamineOn May 18, 2021 ,《Interface-Promoted Direct Oxidation of p-Arsanilic Acid and Removal of Total Arsenic by the Coupling of Peroxymonosulfate and Mn-Fe-Mixed Oxide》 appeared in Environmental Science & Technology. The author of the article were Ke, Ming-Kun; Huang, Gui-Xiang; Mei, Shu-Chuan; Wang, Zhao-Hua; Zhang, Ying-Jie; Hua, Tian-Wei; Zheng, Li-Rong; Yu, Han-Qing. The article conveys some information:

As one of the extensively used feed additives in livestock and poultry breeding, p-arsanilic acid (p-ASA) has become an organoarsenic pollutant with great concern. For the efficient removal of p-ASA from water, the combination of chem. oxidation and adsorption is recognized as a promising process. Herein, hollow/porous Mn-Fe-mixed oxide (MnFeO) nanocubes were synthesized and used in coupling with peroxymonosulfate (PMS) to oxidize p-ASA and remove the total arsenic (As). Under acidic conditions, both p-ASA and total As could be completely removed in the PMS/MnFeO process and the overall performance was substantially better than that of the Mn/Fe monometallic system. More importantly, an interface-promoted direct oxidation mechanism was found in the p-ASA-involved PMS/MnFeO system. Rather than activate PMS to generate reactive oxygen species (i.e., SO4·-, ·OH, and 1O2), the MnFeO nanocubes first adsorbed p-ASA to form a ligand-oxide interface, which improved the oxidation of the adsorbed p-ASA by PMS and ultimately enhanced the removal of the total As. Such a direct oxidation process achieved selective oxidation of p-ASA and avoidance of severe interference from the commonly present constituents in real water samples. After facile elution with dilute alkali solution, the used MnFeO nanocubes exhibited superior recyclability in the repeated p-ASA removal experiments Therefore, this work provides a promising approach for efficient abatement of phenylarsenical-caused water pollution based on the PMS/MnFeO oxidation process.Triacetonamine(cas: 826-36-8Reference of Triacetonamine) was used in this study.

Triacetonamine(cas: 826-36-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Reference of Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Category: piperidinesOn October 6, 2005 ,《Potent Cannabinergic Indole Analogues as Radioiodinatable Brain Imaging Agents for the CB1 Cannabinoid Receptor》 was published in Journal of Medicinal Chemistry. The article was written by Deng, Hongfeng; Gifford, Andrew N.; Zvonok, Alexander M.; Cui, Guangjian; Li, Xiuyan; Fan, Pusheng; Deschamps, Jeffrey R.; Flippen-Anderson, Judith L.; Gatley, S. John; Makriyannis, Alexandros. The article contains the following contents:

A series of novel aminoalkylindoles was synthesized in an effort to develop compounds that are potent agonists at the CB1 cannabinoid receptor and that are also easily labeled with radioisotopes of iodine for biochem. and imaging studies. 2-Iodophenyl-[1-(1-methylpiperidin-2-ylmethyl)-1H-indol-3-yl]methanone I (AM2233) had a very high affinity for the rat CB1 receptor, with most of the affinity residing with the (R)-enantiomer. Radioiodinated racemic I and its enantiomers were prepared by radioiododestannylation of the tributyltin analogs in high yields, radiochem. purities, and specific radioactivities. In a mouse hippocampal membrane preparation with [131I](R)-I as radioligand, racemic I exhibited a Ki value of 0.2 nM compared with 1.6 nM for WIN55212-2. In autoradiog. experiments with mouse brain sections, the distribution of radioiodinated I was consistent with that of brain CB1 receptors. Again, very little specific binding was seen with the (S)-enantiomer [131I](S)-I and none occurred with the (R)-enantiomer [131I](R)-I in sections from CB1 receptor knockout mice. Radioiodinated I thus appears to be a suitable radioligand for studies of CB1 cannabinoid receptors. After reading the article, we found that the author used 1-Methylpiperidine-2-carboxylic acid hydrochloride(cas: 25271-35-6Category: piperidines)

1-Methylpiperidine-2-carboxylic acid hydrochloride(cas: 25271-35-6) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

HPLC of Formula: 126832-81-3On May 19, 2005 ,《Synthesis and Structure-Activity Relationships of Novel Selective Factor Xa Inhibitors with a Tetrahydroisoquinoline Ring》 appeared in Journal of Medicinal Chemistry. The author of the article were Ueno, Hiroshi; Yokota, Katsuyuki; Hoshi, Jun-Ichi; Yasue, Katsutaka; Hayashi, Mikio; Hase, Yasunori; Uchida, Itsuo; Aisaka, Kazuo; Katoh, Susumu; Cho, Hidetsura. The article conveys some information:

A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds I.2HCl and I.MsOH exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, I.MsOH exhibited potent anti-FXa activity after i.v. and oral administration to cynomolgus monkeys, showed a dose-dependent antithrombotic effect at 0.1, 0.3, and 1 mg kg-1 h-1 in a rat model of venous thrombosis, and significantly reduced the size of brain infarction in a middle cerebral artery occlusion model at a dose of 0.1 mg kg-1 h-1. These results suggest that I.MsOH (JTV-803) is likely to be useful as both a venous and arterial antithrombotic agent. The results came from multiple reactions, including the reaction of 1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3HPLC of Formula: 126832-81-3)

1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. HPLC of Formula: 126832-81-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem