Day: October 18, 2022

《Synthesis and Anticancer Activity of New Substituted Piperidinones Linked to Pyrimidine, Thiazole, and Triazole Glycoside Derivatives》 was written by Yousif, M. N. M.; Nassar, I. F.; Yousif, N. M.; Awad, H. M.; El-Sayed, W. A.. Application In Synthesis of Triacetonamine And the article was included in Russian Journal of General Chemistry on August 31 ,2019. The article conveys some information:

New piperidinone incorporating pyrimidine, triazine, diazipine, oxatriazine, and thiazole derivatives have been synthesized starting with tetramethylpipridin-4-one. Structures of the newly synthesized compounds are characterized on the basis of spectroscopic and anal. data. The anticancer activity of the prepared compounds has been studied in vitro against HCT-116 and MCF-7 human cancer cells using the MTT assay. A number of compounds demonstrates potent activity towards both cell lines with IC50 values comparable with doxorubicin. In the experiment, the researchers used Triacetonamine(cas: 826-36-8Application In Synthesis of Triacetonamine)

Triacetonamine(cas: 826-36-8) 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.Application In Synthesis of Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Trichloroacetic acid fueled practical amine purifications》 was published in Beilstein Journal of Organic Chemistry in 2022. These research results belong to Thomas, Aleena; Gasch, Baptiste; Olivieri, Enzo; Quintard, Adrien. Application of 826-36-8 The article mentions the following:

On out of equilibrium mol. machinery, using trichloroacetic acid (TCA), disclosed a purification technique considerably decreasing the number of operations and the waste generation required for such purifications. At first, TCA triggered the precipitation of the amines through their protonated salt formation, enabling the separation with the impurities. From these amine salts, simple decarboxylation of TCA liberated volatile CO2 and chloroform afforded directly the pure amines. Through this approach, a broad range of diversely substituted amines were isolated with success. The experimental part of the paper was very detailed, including the reaction process of Triacetonamine(cas: 826-36-8Application of 826-36-8)

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.Application of 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bai, Rui; Xiao, Yong; Yan, Weifu; Wang, Siqi; Ding, Rui; Yang, Fan; Li, Junpeng; Lu, Xiaoquan; Zhao, Feng published an article in Environmental Science and Pollution Research. The title of the article was 《Rapid and efficient removal of naproxen from water by CuFe2O4 with peroxymonosulfate》.Category: piperidines The author mentioned the following in the article:

Abstract: Naproxen, a widely used nonsteroidal anti-inflammatory drug, has been detected in many environmental matrixes and is regarded as an emerging pollutant. Sulfate radical (SO4·-) -based advanced oxidation processes have attracted wide attention due to their high efficiency and applicability in the removal of emerging contaminants. In this study, CuFe2O4 was used as an efficient catalyst to activate peroxymonosulfate to oxidize naproxen. The results suggested that 92.3% of naproxen was degraded and 50.3% total organic carbon was removed in 60 min in the presence of 0.3 g·L-1 CuFe2O4 and 2 mM peroxymonosulfate. This degradation system showed strong adaptability in a wide pH range from 4.0 to 10.0. Free radical scavenger experiments and ESR anal. indicated that 1O2, ·OH, and SO4·- are the main active species. Finally, the potential degradation pathways of naproxen were proposed by detecting and analyzing the degradation products with ultra-high-performance liquid chromatog. combined with mass spectrometry. The results of this study suggest that the CuFe2O4-activated peroxymonosulfate system is a promising technol. for the removal of naproxen from natural water. The results came from multiple reactions, including the reaction of Triacetonamine(cas: 826-36-8Category: piperidines)

Triacetonamine(cas: 826-36-8) 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

Cheng, Yarui; Zhang, Tianyuan; Cao, Yangrong; Wang, Li; Chen, Wenli published an article in Applied Microbiology and Biotechnology. The title of the article was 《New insights into the function of the proteins IsiC and IsiD from Synechocystis sp. PCC 6803 under iron limitation》.COA of Formula: C6H12N2O The author mentioned the following in the article:

Iron is a common cofactor in biol. processes such as respiration, photosynthesis, and nitrogen fixation. The genes isiC and isiD encode unknown proteins, and the growth of ΔisiC and ΔisiD mutants is inhibited under iron-deficient conditions. To study the regulatory mechanisms of IsiC and IsiD during iron starvation, we carried out transcriptome and metabolome sequencing. The Kyoto Encyclopedia of Genes and Genomes (KEGG) anal. showed that the photosynthesis, nitrogen metabolism, and ABC transporter pathways play a vital role in regulating iron deficiency. Upon iron repletion, IsiC and IsiD also have a regulatory effect on these pathways. Addnl., KEGG anal. of the differential metabolites of wild type (WT) and mutants showed that they were all enriched in starch and sucrose metabolism after iron limitation. Weighted gene co-expression network anal. (WGCNA) constructed a co-expression network of differentially expressed genes with phenotypes and metabolites, and finally identified five modules. The turquoise module was pos. correlated with iron deficiency. In contrast, the WT and blue module exhibited a neg. correlation, and the mutants ΔisiC and ΔisiD were pos. correlated with the gray and brown modules, resp. WGCNA also analyzed the relationship between metabolites and phenotypes, and the green module was related to iron starvation. The co-expression network determined the hub genes and metabolites of each module. This study lays a foundation for a better understanding of cyanobacteria in response to iron deficiency. In addition to this study using Piperidine-4-carboxamide, there are many other studies that have used Piperidine-4-carboxamide(cas: 39546-32-2COA of Formula: C6H12N2O) was used in this study.

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).COA of Formula: C6H12N2O

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Cox, Christopher D.; Coleman, Paul J.; Breslin, Michael J.; Whitman, David B.; Garbaccio, Robert M.; Fraley, Mark E.; Buser, Carolyn A.; Walsh, Eileen S.; Hamilton, Kelly; Schaber, Michael D.; Lobell, Robert B.; Tao, Weikang; Davide, Joseph P.; Diehl, Ronald E.; Abrams, Marc T.; South, Vicki J.; Huber, Hans E.; Torrent, Maricel; Prueksaritanont, Thomayant; Li, Chunze; Slaughter, Donald E.; Mahan, Elizabeth; Fernandez-Metzler, Carmen; Yan, Youwei; Kuo, Lawrence C.; Kohl, Nancy E.; Hartman, George D. published an article in Journal of Medicinal Chemistry. The title of the article was 《Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer》.Recommanded Product: 405057-75-2 The author mentioned the following in the article:

Inhibition of kinesin spindle protein (KSP) is a novel mechanism for treatment of cancer with the potential to overcome limitations associated with currently employed cytotoxic agents. Herein, we describe a C2-hydroxymethyl dihydropyrrole KSP inhibitor (11) that circumvents hERG channel binding and poor in vivo potency, issues that limited earlier compounds from our program. However, introduction of the C2-hydroxymethyl group caused 11 to be a substrate for cellular efflux by P-glycoprotein (Pgp). Utilizing knowledge garnered from previous KSP inhibitors, we found that β-fluorination modulated the pKa of the piperidine nitrogen and reduced Pgp efflux, but the resulting compound (14) generated a toxic metabolite in vivo. Incorporation of fluorine in a strategic, metabolically benign position by synthesis of an N-methyl-3-fluoro-4-(aminomethyl)piperidine urea led to compound 30 that has an optimal in vitro and metabolic profile. Compound 30 (MK-0731) was recently studied in a phase I clin. trial in patients with taxane-refractory solid tumors. The experimental part of the paper was very detailed, including the reaction process of 1-Cbz-4-Methylaminopieridine(cas: 405057-75-2Recommanded Product: 405057-75-2)

1-Cbz-4-Methylaminopieridine(cas: 405057-75-2) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Recommanded Product: 405057-75-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ishihara, Tsukasa; Seki, Norio; Hirayama, Fukushi; Orita, Masaya; Koshio, Hiroyuki; Taniuchi, Yuta; Sakai-Moritani, Yumiko; Iwatsuki, Yoshiyuki; Kaku, Seiji; Kawasaki, Tomihisa; Matsumoto, Yuzo; Tsukamoto, Shin-ichi published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors》.HPLC of Formula: 126832-81-3 The author mentioned the following in the article:

We describe here our investigation of a new series of orally active fXa inhibitors based on a prodrug strategy. Solid-phase parallel synthesis identified a unique series of fXa inhibitors with a substituted benzenesulfonyl group as a novel S4 binding element. This series resulted in compound 39 (I), which exhibited potent inhibitory activity against fXa (IC50 = 13 nM) and excellent selectivity over thrombin (>7000-fold). The masking of its highly hydrophilic groups led to the creation of related prodrug 28, which demonstrated an anticoagulant effect after oral dosing. In addition to this study using 1-Pyridin-4-ylpiperidin-4-one, there are many other studies that have used 1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3HPLC of Formula: 126832-81-3) was used in this study.

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

Li, Zhuoqian; Li, Kai; Ma, Shuanglong; Dang, Bingjun; Li, Yi; Fu, Haichao; Du, Jinge; Meng, Qingxiang published an article on January 15 ,2021. The article was titled 《Activation of peroxymonosulfate by iron-biochar composites: Comparison of nanoscale Fe with single-atom Fe》, and you may find the article in Journal of Colloid and Interface Science.Recommanded Product: 826-36-8 The information in the text is summarized as follows:

A convenient and efficient method to fabricate isolated Fe single-atom catalysts deposited on Myriophyllum aquaticum-based biochar (ISA-Fe/MC) is reported for peroxymonosulfate-based organics degradation Firstly, the Fe nanoparticles anchored on the hierarchical porous biochar (nano-Fe/MC) can be obtained by utilizing K2FeO4 as a synchronous activation and graphitization agent. Subsequently, ISA-Fe/MC was achieved by HCl etching of nano-Fe/MC to remove the excess Fe nanoparticles. Compared with nano-Fe/MC, ISA-Fe/MC demonstrated outperformed catalytic capacity towards PMS activation for phenol degradation The combination of super high surface area, hierarchical porous structure, graphitization structure and atomically dispersed Fe species should be responsible for prominent catalytic oxidation ability and outstanding resistance to common anions and humic acid. Based on the chem. scavengers, EPR experiments and electrochem. tests, the SO•-4 dominated radical degradation pathway for nano-Fe/MC and electron transfer reigned non-radical degradation pathway for ISA-Fe/MC was revealed. In contrast to nano-Fe/MC, d. functional theory calculations demonstrated the enhanced d. of states around Fermi level in ISA-Fe/MC meaning the increased catalytic performance and more electron transfer between single-atom Fe to adjacent graphitic C and N which could serve as electron transfer channel for PMS activation. In the experimental materials used by the author, we found Triacetonamine(cas: 826-36-8Recommanded Product: 826-36-8)

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.Recommanded Product: 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2018,Bioorganic & Medicinal Chemistry Letters included an article by Rong, Rui-Xue; Wang, Shan-Shan; Liu, Xuan; Li, Ren-Feng; Wang, Ke-Rang; Cao, Zhi-Ran; Li, Xiao-Liu. Quality Control of 2-(Piperidin-4-yl)ethanol. The article was titled 《Lysosomes-targeting imaging and anticancer properties of novel bis-naphthalimide derivatives》. The information in the text is summarized as follows:

A series of novel bridged bis-naphthalimide derivatives containing saturated nitrogenous heterocycles were designed and synthesized, their cytotoxic activities against Hela, MCF-7, A549 and MGC-803 cells were investigated. Compounds NI1-NI4 (I.4HCl – IV.4HCl, resp.) modified with piperidine and piperazine exhibited good and selective cytotoxic activity, for instance, compounds NI1 (IC50 2.89 and 0.60 μM) and NI4 (2.73 and 1.60 μM) showed potent cytotoxic activity against Hela cells and MGC-803 cells, resp., better than the control drug (Amonafide). However, compounds conjugated with pyrrole derivatives showed weak cytotoxic activities against the all tested cell lines. Furthermore, their DNA binding properties, fluorescence imaging and cell cycle were investigated. Interestingly, compounds NI1 and NI4 showed fluorescence enhancement because of the strong binding with Ct-DNA, and exhibited fluorescence imaging with Hela cells on the lysosomes. In the part of experimental materials, we found many familiar compounds, such as 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Quality Control of 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.Quality Control of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,European Journal of Medicinal Chemistry included an article by Yao, Bin-Rong; Sun, Yue; Chen, Shuang-Long; Suo, Hao-Dong; Zhang, Yu-Long; Wei, Hao; Wang, Chun-Hua; Zhao, Feng; Cong, Wei; Xin, Wen-Yu; Hou, Gui-Ge. Related Products of 1445-73-4. The article was titled 《Dissymmetric pyridyl-substituted 3,5-bis(arylidene)-4-piperidones as anti-hepatoma agents by inhibiting NF-κB pathway activation》. The information in the text is summarized as follows:

A series of dissym. pyridyl-substituted 3,5-bis(arylidene)-4-piperidones (BAPs, I [R1 = 3-pyridinyl, 4-pyridinyl; R2 = 2-F, 4-cyano, 3,4,5-OMe, etc.] II[R3 = 3-pyridinyl, 4-pyridinyl; R4 = F, CF3; R5 = H, Cl, CF3, etc]) were designed and synthesized to get new anti-hepatoma agents with anti-inflammatory activity and hypotoxicity. Many of them exhibited potential anti-hepatoma properties against human hepatocellular carcinoma cell lines (HepG2, QGY-7703, SMMC-7721) and hypotoxicity for human normal heptical cell line (HHL-5, LO2) and prominently inhibited lipopolysaccharides (LPS) induced IL-6, TNF-α secretion to exert its anti-inflammatory effect. Combining the data of cytotoxicity, cytocompatibility and anti-inflammatory activity, II [R3 = 3-pyridinyl; R4 = R5 = CF3] may be the potential anti-hepatoma agent. II [R3 = 3-pyridinyl; R4 = R5 = CF3] effectively promoted cell apoptosis through up-regulating cleaved caspase-3 and Bax expression and down-regulating Bcl-2 expression. Furthermore, II [R3 = 3-pyridinyl; R4 = R5 = CF3]prominently inhibited NF-κB pathway activation by blocking the phosphorylation of IκBα, p65 and the nuclear translocation of NF-κB induced by TNF-α and LPS. In addition, II [R3 = 3-pyridinyl; R4 = R5 = CF3] could reasonably bind to the active site of Bcl-2 and NF-κB/p65 protein proved by Mol. docking analyses. Moreover, II [R3 = 3-pyridinyl; R4 = R5 = CF3] significantly suppressed the growth and inflammatory response of HepG2 xenografts in nude mice and was relatively nontoxic to mice. These results suggested that II [R3 = 3-pyridinyl; R4 = R5 = CF3] may be effective and hypotoxicity anti-hepatoma agent for the clin. treatment of liver cancers. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-4-piperidone(cas: 1445-73-4Related Products of 1445-73-4)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Related Products of 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Highly durable and conductive poly(arylene piperidine) with a long heterocyclic ammonium side-chain for hydroxide exchange membranes》 were Jin, Cuihong; Zhang, Shuai; Cong, Yuanyuan; Zhu, Xiuling. And the article was published in International Journal of Hydrogen Energy in 2019. Related Products of 1445-73-4 The author mentioned the following in the article:

Recently, the preparation of hydroxide exchange membranes (HEMs) without ether bonds have attracted much attention because of their high chem. stability. Hence, ether-bond free, highly durable, and conductive poly(arylene piperidine)s (PAPips) tethered with heterocyclic ammonium via hexyl spacer chains were prepared successfully for HEMs via a facile synthetic procedure. The effect of the cationic groups (quaternary ammonium, piperidinium, and morpholinium) on the properties of the corresponding PAPip-based HEMs, including the morphol., hydroxide conductivity, and alk. and chem. stability were systematically investigated. The as-designed PAPip-based membranes exhibited excellent overall performance. The membranes attached with piperidinium (IEC = 1.64 mmol g-1) exhibited a hydroxide conductivity of 0.082 S cm-1 at 80°C and exhibited significant alk. stability which maintained 80.1% of its conductivity after immersion in 1 M NaOH at 80°C for 1500 h. The as-prepared membrane also presented a peak power d. of 76 mW cm-2 at 80°C in a H2/O2 HEMFC. The resulting HEMs also showed excellent mech. properties, thermal stability, and well-defined phase separation In the experimental materials used by the author, we found 1-Methyl-4-piperidone(cas: 1445-73-4Related Products of 1445-73-4)

1-Methyl-4-piperidone(cas: 1445-73-4) 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.Related Products of 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem