Day: November 21, 2022

Yu, Valentina K. published the artcileSynthesis and properties of novel alkoxy- and phenoxyalkyl ethers of secondary and tertiary ethynylpiperidin-4-ols possessing unusual analgesic, anti-bacterial, anti-spasmotic, and anti-allergic properties as well as low toxicity, HPLC of Formula: 512778-95-9, the publication is Journal of Saudi Chemical Society (2009), 13(2), 209-217, database is CAplus.

Methodol. was developed to obtain a series of unusual alkoxy- and phenoxyalkyl ethers of secondary and tertiary ethynylpiperidin-4-ols, representative examples of which were evaluated for analgesic, anti-bacterial, anti-spasmotic, and anti-allergic activity. Twenty-two new compounds were prepared and identified by elemental and spectral analyses. Etherification of 4-hydroxypiperidin-4-ols was accomplished via Williamson ether-type syntheses in dry DMF. Side reactions of the bromides used appeared to involve complex processes with DMF under a variety of conditions employed which led to modest yields of products. Since all target mols. were oils at room temperature, conversions to β-cyclodextrins were accomplished and served as vehicles for pharmacol. screening. Several ethynyl-substituted agents displayed deep analgesic activity in the tail flick model, although some alkoxy- and phenoxy ethers from secondary alcs. were less effective as analgesics. Interestingly, LD50 values for the agents exceeded that of a number of clin. agents including Dimedrole, Klemastine, Lidocaine, No-spa, Tramal, Streptomycin, and Euphilline. Three representative examples of the agents exhibited moderate anti-bacterial action against Escherichia coli, Salmonella chloerae suis, Salmonella typhimurium, and Staphylococcus aureus, but did not exceed that of Streptomycin. The absence of the ethynyl ether group resulted in no anti-bacterial activity in several ethers. A few agents possessed anti-spasmotic ability, especially the ethers of 1-(2-ethoxyethyl)-4-ethynyl-4-hydroxypiperidines in various preparations and included the systems of acetylcholine-induced spasms, the histamine-induced spasms, and the calcium chloride-induced spasms. Two examples void of the ethynyl group were not effective as anti-spasmotic compounds A small survey of five agents for anti-allergic properties revealed that two with ethynyl groups were similar in activity with Dimedrole but less than that of Klemastine in screens using acetylcholine and histamine systems. Overall, these families of piperidines possess a wide variety of important biol. properties which require further exploration.

Journal of Saudi Chemical Society published new progress about 512778-95-9. 512778-95-9 belongs to piperidines, auxiliary class Piperidine,Alcohol,Ether, name is 1-(2-Methoxyethyl)piperidin-4-ol, and the molecular formula is C11H15NO2, HPLC of Formula: 512778-95-9.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Qin, Tian published the artcileVinylogous Addition of Siloxyfurans to Benzopyryliums: A Concise Approach to the Tetrahydroxanthone Natural Products, COA of Formula: C11H21BF4N2O2, the publication is Journal of the American Chemical Society (2011), 133(6), 1714-1717, database is CAplus and MEDLINE.

A concise approach to the tetrahydroxanthone natural products employing vinylogous addition of siloxyfurans to benzopyryliums and a late-stage Dieckmann cyclization was developed. With this methodol., chiral, racemic forms of the natural products blennolide B (I) and blennolide C (II) were synthesized in a maximum of four steps from a 5-hydroxychromone substrate. The regio- and diastereoselectivity of the vinylogous additions was probed using computational studies, which suggested the involvement of Diels-Alder-like transition states.

Journal of the American Chemical Society published new progress about 219543-09-6. 219543-09-6 belongs to piperidines, auxiliary class Piperidine,Fluoride,Salt,Amine,Amide, name is 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, and the molecular formula is C11H21BF4N2O2, COA of Formula: C11H21BF4N2O2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Ge, Teng published the artcileGiant enhanced photocatalytic H₂O₂ production over hollow hexagonal prisms carbon nitride, Category: piperidines, the publication is Journal of the Taiwan Institute of Chemical Engineers (2021), 104-111, database is CAplus.

H2O2, as a green and environmentally friendly oxidant, has been widely used in our daily life and industrial production It is of epoch-making significance to develop highly efficient photocatalysts for producing H2O2. In recent years, g-C3N4 has received much attention due to its high chem. stability, environmental friendliness and suitable energy band structure. However, some shortcomings including the fast recombination of photogenerated electron-hole pairs and small sp. surface area in traditional 2D g-C3N4 seriously impede its photocatalytic performance for the production of H2O2.1D hollow nanostructures possess intriguing physicochem. properties and are adopted to overcome the intrinsic shortcomings of g-C3N4. Herein, g-C3N4 with a hollow hexagonal prism structure (CN-HP) is prepared to produce H2O2. It is characterized by XRD, XPS, SEM, HRTEM, ESR and DRS. BET, PL spectra, photocurrent and EIS are used to explain the enhanced photocatalytic performance. Compared with traditional 2D g-C3N4, the sp. surface area of CN-HP increases to 41.513 m²/g, providing more active sites. Meanwhile, its hollow tubular structure can enhance the migration of photogenerated electrons to the catalyst surface, and electrons with a longer lifetime can participate in photocatalytic reactions to achieve high efficiency. The yield of H2O2 production can up to 4.08 μmol over CN-HP in 40 min, which is about 7 times higher than that of traditional 2D g-C3N4, and the apparent quantum efficiency (AQE) of H2O2 production at 420 nm is 2.41%. This research provides a valuable reference for the development of green materials for efficient photocatalytic production of H2O2.

Journal of the Taiwan Institute of Chemical Engineers published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, Category: piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Xu, Rongsong published the artcileSynthesis of β-(1â†?)-oligo-D-mannuronic acid neoglycolipids, COA of Formula: C11H15NOS, the publication is Carbohydrate Research (2008), 343(1), 7-17, database is CAplus and MEDLINE.

Mammalian Toll-like receptors (TLRs) play important roles in host immune defense. The activation of TLR and down-stream signaling pathways have great impact on human physiol. Chem. diverse microbial products as well as synthetic ligands serve as agonists for these receptors. Recently, synthetic TLR ligands are being exploited as useful therapeutic agents for a variety of diseases including infections, inflammatory diseases, and cancers. Alginate polymers and oligosaccharides are strong immune stimulants mediated by TLR2/4, but synthesis of alginate oligomers is rarely studied. Reported here are the design and chem. synthesis of two β-(1â†?)-di- and β-(1â†?)-tri-D-mannuronic acid neoglycolipids I (n = 0, 1) as potential TLR ligands. By using 4,6-di-O-benzylidene-protected 1-thio mannoside as a glycosyl donor, the diastereoselective β-D-mannosylation protocol provides the β-(1â†?)-D-mannobiose and β-(1â†?)-D-mannotriose derivatives, which upon regioselective oxidation with TEMPO/[bis(acetoxy)iodo]benzene (BAIB) oxidation system yield the corresponding β-(1â†?)-D-mannuronic acid containing neoglycolipids I (n = 0, 1).

Carbohydrate Research published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C6H3ClFNO2, COA of Formula: C11H15NOS.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Mao, Shuhua published the artcile(RuBpy₃)²⁺-bisterpyridinyl triangle promoted singlet oxygen (¹O₂) photosensitization for fast oxidation of sulfur mustard simulant, Quality Control of 826-36-8, the publication is Inorganic Chemistry Communications (2022), 109090, database is CAplus.

(RuBpy₃)²⁺-bisterpyridine-based metallacycle T photosensitizer was prepared by a facile single-step self-assembly process. Supramol. self-assembly strategy greatly improved metallacycle T’s photosensitized ability due to its enhanced light-harvesting capability, smaller energy gap (ΔE_ST) between lowest excited singlet state (S1) and lowest excited triplet state (T1) along with excellent solubility which exhibiting higher efficiency for singlet oxygen (¹O₂) production than the ligand L and its pendant [(RuBpy₃)²⁺·2PF₆^–]. In the practical photo-driven degradation of sulfur mustard simulant (2-chloroethyl Et sulfide, CEES), full conversion of toxic CEES to nontoxic CEESO was achieved by metallacycle T with an extremely fast lifetime of 90 s (half lifetime t_1/2 = 25 s) and 100% selectivity (without formation of highly toxic CEESO₂), while ligand L and [(RuBpy₃)²⁺·2PF₆^–] needed 130 s and 330 s, resp. This study demonstrated terpyridine-based novel supermols. can serve as efficient scaffolds for effective enhancement of photosensitization.

Inorganic Chemistry Communications published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, Quality Control of 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Jiang, Baishan published the artcileStructure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma, Recommanded Product: (R,E)-N-(4-(3-((5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide, the publication is European Journal of Medicinal Chemistry (2021), 113481, database is CAplus and MEDLINE.

Development of inhibitors targeting CDK12/13 is of increasing interest as a potential therapy for cancers as these compounds inhibit transcription of DNA damage response (DDR) genes. We previously described THZ531, a covalent inhibitor with selectivity for CDK12/13. In order to elucidate structure-activity relationship (SAR), we have undertaken a medicinal chem. campaign and established a focused library of THZ531 analogs. Among these analogs, BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells. A 3.0 Å co-crystal structure with CDK12/CycK provides a structural rational for selective targeting of Cys1039 located in a C-terminal extension from the kinase domain. With moderate pharmacokinetic properties, BSJ-01-175 exhibits efficacy against an Ewing sarcoma tumor growth in a patient-derived xenograft (PDX) mouse model following 10 mg/kg once a day, i.p. administration. Taken together, BSJ-01-175 represents the first selective CDK12/13 covalent inhibitor with in vivo efficacy reported to date.

European Journal of Medicinal Chemistry published new progress about 1702809-17-3. 1702809-17-3 belongs to piperidines, auxiliary class Cell Cycle,CDK, name is (R,E)-N-(4-(3-((5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide, and the molecular formula is C30H32ClN7O2, Recommanded Product: (R,E)-N-(4-(3-((5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Browne, Christopher M. published the artcileA chemoproteomic strategy for direct and proteome-wide covalent inhibitor target-site identification, HPLC of Formula: 1702809-17-3, the publication is Journal of the American Chemical Society (2019), 141(1), 191-203, database is CAplus and MEDLINE.

Despite recent clin. successes for irreversible drugs, potential toxicities mediated by unpredictable modification of off-target cysteines represents a major hurdle for expansion of covalent drug programs. Understanding the proteome-wide binding profile of covalent inhibitors can significantly accelerate their development; however, current mass spectrometry strategies typically do not provide a direct, amino acid level readout of covalent activity for complex, selective inhibitors. Here we report the development of CITe-Id, a novel chemoproteomic approach that employs covalent pharmacol. inhibitors as enrichment reagents in combination with an optimized proteomic platform to directly quantify dose-dependent binding at cysteine-thiols across the proteome. CITe-Id anal. of our irreversible CDK inhibitor THZ1 identified dose-dependent covalent modification of several unexpected kinases, including a previously unannotated cysteine (C840) on the understudied kinase PKN3. These data streamlined our development of JZ128 as a new selective covalent inhibitor of PKN3. Using JZ128 as a probe compound, we identified novel potential PKN3 substrates, thus offering an initial mol. view of PKN3 cellular activity. CITe-Id provides a powerful complement to current chemoproteomic platforms to characterize the selectivity of covalent inhibitors, identify new, pharmacol. addressable cysteine-thiols, and inform structure-based drug design programs.

Journal of the American Chemical Society published new progress about 1702809-17-3. 1702809-17-3 belongs to piperidines, auxiliary class Cell Cycle,CDK, name is (R,E)-N-(4-(3-((5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide, and the molecular formula is C30H32ClN7O2, HPLC of Formula: 1702809-17-3.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Wang, Yi published the artcileActivation of peroxydisulfate using N-doped carbon-encapsulated Ni species for efficient degradation of tetracycline, Computed Properties of 826-36-8, the publication is Separation and Purification Technology (2021), 119369, database is CAplus.

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.

Separation and Purification Technology published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C7H7IN2O, Computed Properties of 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Heuckendorff, Mads published the artcileOn the Gluco/Manno Paradox: Practical α-Glucosylation by NIS/TfOH Activation of 4,6-O-Tethered Thioglucoside Donors, COA of Formula: C11H15NOS, the publication is European Journal of Organic Chemistry (2016), 2016(30), 5136-5145, database is CAplus.

A practical protocol for obtaining α-glucosides was established. It was found that 4,6-O-benzylidene or 4,6-O-(di-tert-butylsilylene) tethering of glucosyl donors of the thioglycoside type enables highly α-selective glucosylation under conditions of N-iodosuccinimide (NIS)/triflic acid (TfOH) activation. The α-glucosylation were further found to be largely independent of promoter system, temperature, leaving group and anomeric configuration. The results are discussed in the context of the Glucose/Mannose paradox in glycosylation chem.

European Journal of Organic Chemistry published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C11H15NOS, COA of Formula: C11H15NOS.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Crich, David published the artcileStereocontrolled Formation of β-Glucosides and Related Linkages in the Absence of Neighboring Group Participation: Influence of a trans-Fused 2,3-O-Carbonate Group, Related Products of piperidines, the publication is Journal of Organic Chemistry (2005), 70(18), 7252-7259, database is CAplus and MEDLINE.

Ph 4,6-di-O-benzyl-2,3-O-carbonyl-β-D-glucothiopyranoside and the regio-isomeric Ph 2,6-di-O-benzyl-3,4-O-carbonyl-β-D-glucothiopyranoside were prepared and studied as glucosyl donors at -60 °C in dichloromethane with pre-activation by 1-benzenesulfinyl piperidine before addition of the acceptor alc. The 2,3-O-carbonate protected donor showed moderate to excellent β-selectivity under these conditions depending on the acceptor employed, thereby providing a means for 1,2-trans-equatorial glycosidic bonds without recourse to neighboring group participation and its associated problem of ortho ester formation. In contrast, the 3,4-O-carbonate protected donor showed moderate to no β-selectivity under the conditions employed. The results obtained in this study with carbonate protected glucopyranosyl donors are contrasted with those obtained previously in the manno- and rhamnopyranosyl series when the 2,3-O-carbonate protected is α-selective and the 3,4-O-carbonate is β-selective.

Journal of Organic Chemistry published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C11H15NOS, Related Products of piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem