Month: October 2022

Sternfeld, Francine; Baker, Raymond; Broughton, Howard B.; Guiblin, Alexander R.; Jelley, Richard A.; Matassa, Victor G.; Reeve, Austin J.; Beer, Margaret; Stanton, Josephine a. published their research in Bioorganic & Medicinal Chemistry Letters on August 6 ,1996. The article was titled 《The chemical evolution of N,N-dimethyl-2-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]ethylamine (L-741,604) and analogs: potent and selective agonists for 5-HT1D receptors》.Reference of Methyl 2-(1-methylpiperidin-4-yl)acetate The article contains the following contents:

Optimization of a series of 5-(heterocyclyl)tryptamines led to the identification of the sym. substituted, N-4 linked 1,2,4-triazole as the best indole C-5 substituent for 5-HT1D receptor affinity and selectivity. The triazole I is the most potent and selective, orally bioavailable, 5-HT1D receptor agonist identified to date, showing an order of magnitude greater potency than the clin. compound sumatriptan with improved subtype selectivity. The experimental part of the paper was very detailed, including the reaction process of Methyl 2-(1-methylpiperidin-4-yl)acetate(cas: 95533-25-8Reference of Methyl 2-(1-methylpiperidin-4-yl)acetate)

Methyl 2-(1-methylpiperidin-4-yl)acetate(cas: 95533-25-8) 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.Reference of Methyl 2-(1-methylpiperidin-4-yl)acetate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer’s disease》 were Mo, Jun; Chen, Tingkai; Yang, Hongyu; Guo, Yan; Li, Qi; Qiao, Yuting; Lin, Hongzhi; Feng, Feng; Liu, Wenyuan; Chen, Yao; Liu, Zongliang; Sun, Haopeng. And the article was published in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020. Recommanded Product: 39546-32-2 The author mentioned the following in the article:

Cholinesterase inhibitor plays an important role in the treatment of patients with Alzheimer’s disease (AD). Herein, we report the medicinal chem. efforts leading to a new series of 1,3-dimethylbenzimidazolinone derivatives Among the synthesized compounds, and showed submicromolar IC50 values (, eeAChE IC50 = 0.39 ± 0.11μM; , eqBChE IC50 = 0.16 ± 0.04μM) towards acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Kinetic and mol. modeling studies revealed that and act in a competitive manner. and showed neuroprotective effect against H2O2-induced oxidative damage on PC12 cells. This effect was further supported by their antioxidant activity determined in a DPPH assay in vitro. Morris water maze test confirmed the memory amelioration effect of the two compounds in a scopolamine-induced mouse model. Moreover, the hepatotoxicity of and was lower than tacrine. In summary, these data suggest and are promising multifunctional agents against AD. The results came from multiple reactions, including the reaction of Piperidine-4-carboxamide(cas: 39546-32-2Recommanded Product: 39546-32-2)

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).Recommanded Product: 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhang, Zhe; Zhang, Zhao-Sheng; Wang, Xiao; Xi, Gao-Lei; Jin, Zhen; Tang, You-Zhi published an article in 2021. The article was titled 《A click chemistry approach to pleuromutilin derivatives, evaluation of anti-MRSA activity and elucidation of binding mode by surface plasmon resonance and molecular docking》, and you may find the article in Journal of Enzyme Inhibition and Medicinal Chemistry.Quality Control of 2-(Piperidin-4-yl)ethanol The information in the text is summarized as follows:

A series of pleuromutilin analogs containing substituted 1,2,3-triazole moieties I [R1 = Me, Ph, 3-fluorophenyl, etc.] and II [R2 = R3 = Me, cyclohexyl, etc.] were designed, synthesized and assessed for their in vitro antibacterial activity against Methicillin-resistant Staphylococcus aureus (MRSA). Initially, the in vitro antibacterial activities of these derivatives against 4 strains of S. aureus (MRSA ATCC 43300, ATCC 29213, AD3, and 144) were tested by the broth dilution method. Most of the synthesized pleuromutilin analogs displayed potent activities. Among them, compounds I [R1 = 2-methylphenyl, 2-nitrophenyl, 4-nitrophenyl] (MIC = 0.5∼1 μg/mL) showed the most effective antibacterial activity and their anti-MRSA activity were further studied by the time-killing kinetics approach. Binding mode investigations by surface plasmon resonance (SPR) with 50S ribosome revealed that the selected compounds all showed obvious affinity for 50S ribosome (KD = 2.32 x 10-8∼5.10 x 10-5 M). Subsequently, the binding of compounds I [R1 = 2-methylphenyl, 4-nitrophenyl] to the 50S ribosome was further investigated by mol. modeling. Compound I [R1 = 2-methylphenyl] had a superior docking mode with 50S ribosome, and the binding free energy of compound was calculated to be -12.0 kcal/mol. In the experiment, the researchers used many compounds, for example, 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) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKQuality Control of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Fe3O4 supported on water caltrop-derived biochar toward peroxymonosulfate activation for urea degradation: the key role of sulfate radical》 was written by Li, Guang; Cao, Xiao-qiang; Meng, Na; Huang, Yi-meng; Wang, Xu-dong; Gao, Yuan-yuan; Li, Xuan; Yang, Ting-shu; Li, Bo-lai; Zhang, Yi-zhen; Lyu, Xian-jun; Liang, Yue. Computed Properties of C9H17NO And the article was included in Chemical Engineering Journal (Amsterdam, Netherlands) on April 1 ,2022. The article conveys some information:

A new type of iron-doped and porous biochar (Fe@BC) derived from water caltrop was systematically investigated to catalyze the organic pollutants degradation by peroxymonosulfate (PMS). The effectiveness of this novel material was tested by treating excessive urea concentrations in swimming pool water. It exhibited good PMS activation capacity, achieving urea removal of 100% within 15 min. The Fe@BC/PMS system exhibited excellent resistance to common anions. Only chloride showed a small inhibitory effect, and the removal efficiency of urea decreased by 10% ([Cl-]0 = 10 mM). Quenching experiments and ESR spectroscopy analyses demonstrated that urea degradation was mainly mediated by the radical pathway, which in turn was dominated by surface-bound sulfate radicals (SO4·-). Further, reusability experiments confirmed the stability of the material. After three cycles, the degradation efficiency can still reach 86%. Therefore, the conversion of water caltrop-derived biochar into a composite catalytic material provides a novel strategy for value-added utilization of aquatic waste biomass, and it is also a promising alternative for the treatment of urea from swimming pool water.Triacetonamine(cas: 826-36-8Computed Properties of C9H17NO) was used in this study.

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.Computed Properties of C9H17NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《The action of tertiary and quaternary arecaidine and dihydroarecaidine esters on the guinea pig isolated ileum》 was published in British Journal of Pharmacology and Chemotherapy in 1966. These research results belong to Gloge, Holger; Luellmann, Heinz; Mutschler, Erich. COA of Formula: C8H15NO2 The article mentions the following:

A homologous series of tertiary and quaternary arecaidine esters (methyl to isobutyl), as well as the corresponding dihydrocompds., were investigated quant. on the isolated ileum of the guinea pig. The tertiary arecaidine esters are agonists. Highest activities (effective doses) are observed for the Et ester (E.D.50 = 1.5 × 10-4M) and for arecoline, the Me ester (E.D.50 = 5.8 × 10-8M). Esters with a longer side-chain show considerably lower activity. The intrinsic activities of arecaidine Et ester, arecoline, and dimethylaminoethyl acetate are higher than that of acetylcholine. Hydrogenation of the double bond in the ring markedly reduces the affinity and intrinsic activity of the tertiary arecaidine esters. Hydrogenated esters with a longer side-chain act as inhibitors. Quaternization by means of iodomethylation exerts varying influences on the intrinsic activities of arecaidine esters. In the case of the Me ester the intrinsic activity is somewhat reduced whereas that of the Et ester considerably decreases upon iodomethylation, thus yielding a partial antagonist. Similar transformation of esters with a longer side-chain leads to a complete loss of intrinsic activity. The quaternized compounds thus obtained are inhibitors with atropine-like action. Iodoethylation and iodopropylation even abolish the intrinsic activities of esters with a short side-chain. Hydrogenation of the double bond in the ring of the quaternary compounds similarly diminishes the activity as observed for the tertiary compounds For aliphatic N atoms, quaternization is essential in order to enable a reaction with the acetylcholine receptors of the muscarine type. In the case of ring N atoms, the tertiary protonated form is necessary for obtaining a high intrinsic activity upon combination with the receptor mol. In arecaidine esters, quaternization of the ring N atom reduces or even destroys intrinsic activity, in proportion to the length of the ester side-chain. The experimental process involved the reaction of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8COA of Formula: C8H15NO2)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) 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.COA of Formula: C8H15NO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

COA of Formula: C7H11NO4On September 15, 1993 ,《Characterization of [35S]lanthionine ketimine specific binding to bovine brain membranes》 was published in Biochemical and Biophysical Research Communications. The article was written by Dupre, S.; Fontana, M.; Costa, M.; Pecci, L.; Ricci, G.; Cavallini, D.. The article contains the following contents:

[35S]Lanthionine ketimine binds specifically and with high affinity to bovine brain membranes. This binding has been studied in detail. It is reversible, not occurring at an uptake site or at a metabolizing enzyme and depending only weakly on ionic strength; it is affected by thiol reagents. [35S]Lanthionine ketimine specific binding is displaced only by other ketimines and by catecholamines, but not by more selective adrenergic ligands; binding parameters are reported. [3H]Adrenaline but not [3H]dihydroalprenolol is partially displaced by lanthionine ketimine. With bovine brain preparations a significant stimulation of basal adenylate cyclase activity by lanthionine ketimine is observedCis-piperidine-2,6-dicarboxylic acid(cas: 59234-40-1COA of Formula: C7H11NO4) was used in this study.

Cis-piperidine-2,6-dicarboxylic acid(cas: 59234-40-1) 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.COA of Formula: C7H11NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Product Details of 826-36-8On March 5, 2022, Wang, Gen; Ge, Lei; Liu, Zhuoyue; Zhu, Xiurong; Yang, Shengjiong; Wu, Kun; Jin, Pengkang; Zeng, Xiangkang; Zhang, Xiwang published an article in Chemical Engineering Journal (Amsterdam, Netherlands). The article was 《Activation of peroxydisulfate by defect-rich CuO nanoparticles supported on layered MgO for organic pollutants degradation: An electron transfer mechanism》. The article mentions the following:

Heterogeneous activation of peroxydisulfate (PDS) by transition metal oxides offers a promising strategy for organic pollutants removal but suffers from low electron transfer efficiency. Herein, layered MgO supported CuO nanoparticles was prepared by thermal conversion of metal-phenolic networks of Cu2+/Mg2+ and tannic acid. CuO nanoparticles (≈2 nm) were spatial monodispersed on layered MgO, inducing the formation of electron deficient Cu3+ and surface oxygen vacancies and thus facilitated adsorption and activation of PDS. The electron-rich CuO/MgO hybrid catalysts manifested good catalytic performance of PDS activation for organic pollutants removal. At 0.18 g/L of CuO/MgO hybrid catalyst and 0.2 mM of PDS, complete removal of bisphenol A (BPA) was achieved with a high kinetic constant (0.1 min-1, 50 min). Quenching experiments, ESR tests, PDS decomposition behaviors, electrochem. anal. and in situ ATR-FTIR and Raman spectroscopy revealed a nonradical pathway of electron transfer for PDS activation. The CuO/MgO hybrid catalysts exhibited wide working pH range from 3 to 11, selective oxidation capability, good resistance to halide ion and high utilization efficiency of PDS, and thus would be a promising candidate for wastewater remediation. The experimental part of the paper was very detailed, including the reaction process of Triacetonamine(cas: 826-36-8Product Details of 826-36-8)

Triacetonamine(cas: 826-36-8) 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.Product Details of 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthetic Route of C9H17NOOn March 1, 2022, Wei, Ying; Lu, Guanglu; Xie, Dongrun; Sun, Tianyi; Liu, Yu; Zhang, Ying; An, Jiutao; Li, Menghong; Guo, He published an article in Chemical Engineering Journal (Amsterdam, Netherlands). The article was 《Degradation of enrofloxacin in aqueous by DBD plasma and UV: Degradation performance, mechanism and toxicity assessment》. The article mentions the following:

Enrofloxacin (ENRO) as a highly toxic antibiotic poses great threats to human health and environmental safety. In this study, a novel technol. of coupling dielec. barrier discharge (DBD) and UV was investigated to efficiently degrade ENRO in aqueous, and had a higher degradation rate. The ENRO degradation rate achieved approx. 93.9% at 30 min, and approx. 1.20 g kWh-1 of energy yield (G50) was observed for the combined system. The addition of H2O2 and K2S2O4 improved the ENRO degradation due to the generation of ·OH and ·SO42-. In the presence of NO3-, the ENRO degradation played a tendency to promote first and then decrease, and the presence of SO42-resulted in the pos. effect, while the neg. effect was shown in the presence of Cl- and CO32-. The trapping experiment indicated that ·OH played an important part in the ENRO degradation The addition of UV into the DBD system decreased H2O2 concentration in deionized water, and increased ·OH concentration The DFT anal. showed the degradation mechanisms of ENRO at a mol. level. The degradation of ENRO mainly involved the oxidation of the piperazine group, the removal of Et acetate and the substitution of the F atom. The toxicity of ENRO and its degradation intermediates was evaluated. After reading the article, we found that the author used Triacetonamine(cas: 826-36-8Synthetic Route of C9H17NO)

Triacetonamine(cas: 826-36-8) 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.Synthetic Route of C9H17NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Sun, Ping; Liu, Hui; Zhai, Zhicai; Zhang, Xuesheng; Fang, Yingsen; Tan, Jun; Wu, Jiaqiang published an article on January 15 ,2019. The article was titled 《Degradation of UV filter BP-1 with nitrogen-doped industrial graphene as a metal-free catalyst of peroxymonosulfate activation》, and you may find the article in Chemical Engineering Journal (Amsterdam, Netherlands).Application In Synthesis of Triacetonamine The information in the text is summarized as follows:

Instead of previously reported graphene oxide (GO), industrial graphene (reduced graphene oxide (IrGO)) was annealed with a nitrogen precursor. The obtained nitrogen-doped graphene (N-IrGO) was then employed as a novel catalyst for peroxymonosulfate (PMS) activation to degrade benzophenone-1 (BP-1) for the first time. The results show that N-IrGO exhibits excellent catalytic performance over conventional GO and its nitrogen-doped sample and was even better than the metal catalysts Co3O4 and Fe3O4. The enhanced catalytic performance might be attributed to graphitic-like nitrogen. Moreover, the effects of various factors were studied, including catalyst load, PMS concentration and reaction temperature Possible degradation pathways of BP-1 in the N-IrGO/PMS system were proposed based on detected intermediates and the frontier electron d. calculation Radical quenching experiments and ESR (EPR) tests indicated that nonradical oxidation (singlet oxygen (1O2)) plays a dominant role in the BP-1 degradation, in contrast to the previously proposed radical process. Finally, mineralization and stability experiments confirmed that N-IrGO may be an alternative catalyst for environmental remediation. This study contributes to designing novel graphene materials with N doping and gives new insight into nonradical oxidation on benzophenone-type UV filters degradation The results came from multiple reactions, including the reaction of Triacetonamine(cas: 826-36-8Application In Synthesis 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.Application In Synthesis of Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2014,Vidadala, Rama Subba Rao; Ojo, Kayode K.; Johnson, Steven M.; Zhang, Zhongsheng; Leonard, Stephen E.; Mitra, Arinjay; Choi, Ryan; Reid, Molly C.; Keyloun, Katelyn R.; Fox, Anna M. W.; Kennedy, Mark; Silver-Brace, Tiffany; Hume, Jen C. C.; Kappe, Stefan; Verlinde, Christophe L. M. J.; Fan, Erkang; Merritt, Ethan A.; Van Voorhis, Wesley C.; Maly, Dustin J. published 《Development of potent and selective Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) inhibitors that block the transmission of malaria to mosquitoes》.European Journal of Medicinal Chemistry published the findings.COA of Formula: C7H15NO The information in the text is summarized as follows:

Malaria remains a major health concern for a large percentage of the world’s population. While great strides have been made in reducing mortality due to malaria, new strategies and therapies are still needed. Therapies that are capable of blocking the transmission of Plasmodium parasites are particularly attractive, but only primaquine accomplishes this, and toxicity issues hamper its widespread use. In this study, the authors describe a series of pyrazolopyrimidine- and imidazopyrazine-based compounds that are potent inhibitors of PfCDPK4, which is a calcium-activated Plasmodium protein kinase that is essential for exflagellation of male gametocytes. Thus, PfCDPK4 is essential for the sexual development of Plasmodium parasites and their ability to infect mosquitoes. The authors demonstrate that two structural features in the ATP-binding site of PfCDPK4 can be exploited to obtain potent and selective inhibitors of this enzyme. Furthermore, the authors demonstrate that pyrazolopyrimidine-based inhibitors that are potent inhibitors of the in vitro activity of PfCDPK4 are also able to block Plasmodium falciparum exflagellation with no observable toxicity to human cells. This medicinal chem. effort serves as a valuable starting point in the development of safe, transmission-blocking agents for the control of malaria. In the experiment, the researchers used many compounds, for example, 2-(Piperidin-4-yl)ethanol(cas: 622-26-4COA of Formula: C7H15NO)

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 FAKCOA of Formula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem