Day: October 21, 2022

Chen, Nanjun; Paek, Sae Yane; Lee, Ju Yeon; Park, Jong Hyeong; Lee, So Young; Lee, Young Moo published their research in Energy & Environmental Science in 2021. The article was titled 《High-performance anion exchange membrane water electrolyzers with a current density of 7.68 A cm-2 and a durability of 1000 hours》.Formula: C6H11NO The article contains the following contents:

Low-cost anion exchange membrane (AEM) water electrolyzers (AEMWEs) are a new technol. for the production of high-purity hydrogen; however, their c.d. and durability are far lower than those of proton exchange membrane water electrolyzers (PEMWEs). Here, we report poly(fluorenyl-co-aryl piperidinium) (PFAP)-based anhydrous cathode AEMWEs that exceed the state-of-the-art PEMWEs with respect to c.d. In addition to a rational electrode design, PFAP-based AEMs with a high water diffusivity and ion conductivity are crucial for high-performance AEMWEs. Using platinum-group-metal (PGM) catalysts, the present AEMWEs achieved a new record c.d. of 7.68 A cm-2 at 2.0 V with a 1 M KOH anode, which surpasses that of state-of-the-art PEMWEs (6 A cm-2 at 2.0 V). PGM-free AEMWEs displayed an excellent c.d. of 1.62 A cm-2 at 2.0 V. Importantly, PGM and PGM-free AEMWEs operated stably under a 0.5 A cm-2 c.d. at 60 °C for more than 1000 h. This work sheds light on current high-performance AEMWEs. In the experiment, the researchers used many compounds, for example, 1-Methyl-4-piperidone(cas: 1445-73-4Formula: C6H11NO)

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.Formula: C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Category: piperidinesIn 2019 ,《Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC)》 appeared in Journal of Medicinal Chemistry. The author of the article were Wang, Wentian; Zhang, Lu; Morlock, Lorraine; Williams, Noelle S.; Shay, Jerry W.; De Brabander, Jef K.. The article conveys some information:

Despite advances in targeted anticancer therapies, there are still no small-mol.-based therapies available that specifically target colorectal cancer (CRC) development and progression, the second leading cause of cancer deaths. We previously disclosed the discovery of truncating adenomatous polyposis coli (APC)-selective inhibitor 1 (TASIN-1), a small mol. that specifically targets colorectal cancer cells lines with truncating mutations in the adenomatous polyposis coli (APC) tumor suppressor gene through inhibition of cholesterol biosynthesis. Here, we report a medicinal chem. evaluation of a collection of TASIN analogs and activity against colon cancer cell lines and an isogenic cell line pair reporting on the status of APC-dependent selectivity. A number of potent and selective analogs were identified, including compounds with good metabolic stability and pharmacokinetic properties. The compounds reported herein represent a first-in-class genotype-selective series that specifically target apc mutations present in the majority of CRC patients and serve as a translational platform toward a targeted therapy for colon cancer. The results came from multiple reactions, including the reaction of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Category: piperidines)

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 FAKCategory: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Formula: C7H15NOIn 2016 ,《Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase》 appeared in Journal of Medicinal Chemistry. The author of the article were Fraser, Craig; Dawson, John C.; Dowling, Reece; Houston, Douglas R.; Weiss, Jason T.; Munro, Alison F.; Muir, Morwenna; Harrington, Lea; Webster, Scott P.; Frame, Margaret C.; Brunton, Valerie G.; Patton, E. Elizabeth; Carragher, Neil O.; Unciti-Broceta, Asier. The article conveys some information:

Novel pyrazolopyrimidines displaying high potency and selectivity toward SRC family kinases have been developed by combining ligand-based design and phenotypic screening in an iterative manner. Compounds were derived from the promiscuous kinase inhibitor PP1 to search for analogs that could potentially target a broad spectrum of kinases involved in cancer. Phenotypic screening against MCF7 mammary adenocarcinoma cells generated target-agnostic structure-activity relationships that biased subsequent designs toward breast cancer treatment rather than to a particular target. This strategy led to the discovery of two potent antiproliferative leads with phenotypically distinct anticancer mode of actions. Kinase profiling and further optimization resulted in eCF506, the first small mol. with subnanomolar IC50 for SRC that requires 3 orders of magnitude greater concentration to inhibit ABL. eCF506 exhibits excellent water solubility, an optimal DMPK profile and oral bioavailability, halts SRC-associated neuromast migration in zebrafish embryos without inducing life-threatening heart defects, and inhibits SRC phosphorylation in tumor xenografts in mice. In the experimental materials used by the author, we found 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Formula: 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 FAKFormula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Product Details of 1445-73-4In 2020 ,《Quinoline Based Monocarbonyl Curcumin Analogs as Potential Antifungal and Antioxidant Agents: Synthesis, Bioevaluation and Molecular Docking Study》 appeared in Chemistry & Biodiversity. The author of the article were Nagargoje, Amol A.; Akolkar, Satish V.; Siddiqui, Madiha M.; Subhedar, Dnyaneshwar D.; Sangshetti, Jaiprakash N.; Khedkar, Vijay M.; Shingate, Bapurao B.. The article conveys some information:

In search for new fungicidal and free radical scavenging agents, we synthesized a focused library of 2-chloroquinoline based monocarbonyl analogs of curcumin (MACs). The synthesized MACs were evaluated for in vitro antifungal and antioxidant activity. The antifungal activity was evaluated against five different fungal strains such as Candida albicans, Fusarium oxysporum, Aspergillus flavus, Aspergillus niger, and Cryptococcus neoformans, resp. Most of the synthesized MACs displayed promising antifungal activity compared to the standard drug Miconazole. Furthermore, mol. docking study on a crucial fungal enzyme sterol 14α-demethylase (CYP51) could provide insight into the plausible mechanism of antifungal activity. MACs were also screened for in vitro radical scavenging activity using butylated hydroxytoluene (BHT) as a standard Almost all MACs exhibited better antioxidant activity compared to BHT. After reading the article, we found that the author used 1-Methyl-4-piperidone(cas: 1445-73-4Product Details 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.Product Details of 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Molecular modeling of three-dimensional structure of hTRPV4 protein and experimental verification of its antagonist binding sites》 was written by Ai, Chongyi; Zhang, Wenjuan; Zhou, Lulu; Cai, Xu; Zheng, Zhibing. Computed Properties of C10H20N2O2This research focused onTRPV4 protein inhibitor synthesis binding modeling acute lung injury. The article conveys some information:

The transient receptor potential vanilloid type 4 (TRPV4) is a polymodal receptor. Antagonists of human TRPV4 (hTRPV4) represent a novel therapeutic approach for acute lung injury (ALI). However, the discovery of various hTRPV4 antagonists has been difficult due to the unavailability of 3D-structure of hTRPV4 protein. We constructed the 3D-structure of hTRPV4 protein by homol. modeling, and the binding pocket of antagonist with hTRPV4 was predicted for the first time. The pocket was consistent with the same subfamily rabbit TRPV5. The detailed interactions of different protein-ligand complexes were calculated by mol. docking and mol. dynamics (MD) simulation, and the outcome revealed the rationality of the binding pocket. Based on the docking and MD results of this model and the structure of compound A2, a TRPV4 antagonist reported in literature, two small mol. compounds, B1 and B2, were designed and synthesized as hTRPV4 antagonists. The results of biol. evaluation in vitro showed that these compounds have good inhibitory activity on hTRPV4. Moreover, the results were in good agreement with those predicted by mol. simulation, which in turn suggested that the modeling 3D structure and the predicted active sites of hTRPV4 are reasonable and reliable. The compound B2, with novel structure and potent inhibitory activity against hTRPV4, can be a promising lead compound for discovering new hTRPV4 antagonists in the future. In addition to this study using tert-Butyl 4-aminopiperidine-1-carboxylate, there are many other studies that have used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Computed Properties of C10H20N2O2) was used in this study.

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Computed Properties of C10H20N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Optical resolution of amino acid derivatives by high-performance liquid chromatography on tris(phenylcarbamate)s of cellulose and amylose》 was written by Okamoto, Yoshio; Kaida, Yuriko; Aburatani, Ryo; Hatada, Koichi. Formula: C16H21NO4 And the article was included in Journal of Chromatography on August 30 ,1989. The article conveys some information:

The optical resolution of 10 N-protected alanine esters was examined by HPLC using 6 cellulose and 5 amylose tris(phenylcarbamate) derivatives as chiral stationary phases. Tris(3,5-dimethylphenylcarbamate)s of both cellulose and amylose showed high resolving power for these racemates. The resolution of 23 N-benzyloxycarbonyl α-amino acid ester was also tested on tris(3,5-dimethylphenylcarbamate)s of cellulose and amylose. All but 2 amino acid derivatives were completely resolved at least by one of the columns. On cellulose tris(3,5-dimethylphenylcarbamate), all L-amino acids (except threonine) eluted first. In the experiment, the researchers used 1-Benzyl 2-ethyl piperidine-1,2-dicarboxylate(cas: 126401-22-7Formula: C16H21NO4)

1-Benzyl 2-ethyl piperidine-1,2-dicarboxylate(cas: 126401-22-7) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Formula: C16H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Recommanded Product: 136624-42-5On June 13, 2016, Stotani, Silvia; Lorenz, Christoph; Winkler, Matthias; Medda, Federico; Picazo, Edwige; Ortega Martinez, Raquel; Karawajczyk, Anna; Sanchez-Quesada, Jorge; Giordanetto, Fabrizio published an article in ACS Combinatorial Science. The article was 《Design and Synthesis of Fsp3-Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening》. The article mentions the following:

The exploration of innovative chem. space is a critical step in the early phases of drug discovery. Bis-spirocyclic frameworks occur in natural products and other biol. relevant metabolites and show attractive features, such as mol. compactness, structural complexity, and three-dimensional character. A concise approach to the synthesis of bis-spirocyclic-based compound libraries starting from readily available com. reagents and robust chem. transformations has been developed. A number of novel bis-spirocyclic scaffold examples, as implemented in the European Lead Factory project, is presented. The experimental process involved the reaction of 4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5Recommanded Product: 136624-42-5)

4-Amino-1-benzylpiperidine-4-carbonitrile(cas: 136624-42-5) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Recommanded Product: 136624-42-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Product Details of 59234-40-1On September 30, 1982 ,《The effects of cyclic dicarboxylic acids on spontaneous and amino acid-evoked activity of rat cortical neurons》 was published in British Journal of Pharmacology. The article was written by Birley, S.; Collins, J. F.; Perkins, M. N.; Stone, T. W.. The article contains the following contents:

At relatively low ejecting currents (10-25 nA), cis-2,3-piperidinedicarboxylic acid (I) [46026-75-9] had no effect on spontaneous firing in neurons of rat cerebral cortex, but selectively antagonized the excitation evoked by N-methyl-D-aspartate (II) without affecting responses to quisqualate or kainate. At higher ejecting currents (60-100 nA), responses to all 3 agonists were reduced. Other cis-piperidinedicarboxylic acids and piperazine-2,3-dicarboxylic acid  [84619-47-6] had only weak and variable effects on cell firing and responses to II, quisqualate, kainate, glutamate, and aspartate. Excitation was produced by 2,3-pyridinedicarboxylic acid (quinolinic acid) [89-00-9] in all cortical neurons tested. Thus, quinolinic acid may be of physiol. interest as a potential endogenous excitant in the nervous system and I and its N-Me derivative may be of use in studies of receptor pharmacol. and the identification of synaptic transmitters. In the experiment, the researchers used many compounds, for example, Cis-piperidine-2,6-dicarboxylic acid(cas: 59234-40-1Product Details of 59234-40-1)

Cis-piperidine-2,6-dicarboxylic acid(cas: 59234-40-1) 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.Product Details of 59234-40-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

COA of Formula: C9H17NOOn September 22, 2021 ,《Tuning reaction pathways of peroxymonosulfate-based advanced oxidation process via defect engineering》 was published in Cell Reports Physical Science. The article was written by Huang, Renfeng; Zhu, Yunmin; Curnan, Matthew T.; Zhang, Yongqing; Han, Jeong Woo; Chen, Yan; Huang, Shaobin; Lin, Zhang. The article contains the following contents:

Peroxymonosulfate (PMS)-based advanced oxidation process (AOP) has attracted great attention as an effective technique for oxidatively decomposing organic pollutants. The PMS activation mechanisms, nevertheless, are still ambiguous in many cases, and, thus, controlling PMS activation pathways for efficient pollutant removal remains challenging. In this work, taking defective PrBa0.5Sr0.5Co1.5Fe0.5O5+v (PBSCF) as a model system, we demonstrate that oxygen vacancies (V•bulo) strongly promote PMS-based AOP, and PMS activation pathways are effectively tuned. Excessive V•bulos are found to modify the surface charge distribution, change PMS adsorption configuration, and break the S-O bond of PMS. As a result, the radical process is promoted, and the predominant nonradical activation pathway shifts from an electron transfer process to singlet oxygen formation. Our mechanistic understanding can guide the rational design of catalysts for efficient water remediation. In the part of experimental materials, we found many familiar compounds, such as Triacetonamine(cas: 826-36-8COA of Formula: 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.COA of Formula: C9H17NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Avery, E. E.; Baevsky, M. F.; Braswell, S. J.; Duffus, C. W.; Evans, G. O. II; Rocha, D. K.; Wynne, R. A. published their research in Journal of Molecular Catalysis on August 1 ,1989. The article was titled 《Palladium phosphine-catalyzed hydroesterifications of unsaturated nitrogen heterocycles》.Reference of Methyl 1-methylpiperidine-3-carboxylate The article contains the following contents:

Pd(PPh3)2Cl2-catalyzed hydroesterification of HCl salts of 1,2,3,6-tetrahydropyridine derivatives gave 37-95% conversion to mixtures of isomeric Me esters. E.g., treatment of N-carbethoxynortropidine with CO-MeOH in MeCOEt containing Pd(PPh3)2Cl2 gave 95% conversion to mainly 3- and 4-(carbomethoxy)isomers I and II, resp., in 1:1.5 ratio. The experimental part of the paper was very detailed, including the reaction process of Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Reference of Methyl 1-methylpiperidine-3-carboxylate)

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.Reference of Methyl 1-methylpiperidine-3-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem