Day: November 21, 2022

Sheppard, Daniel J. published the artcileComparison of disaccharide donors for heparan sulfate synthesis: uronic acids vs. their pyranose equivalents, HPLC of Formula: 4972-31-0, the publication is Organic & Biomolecular Chemistry (2020), 18(25), 4728-4733, database is CAplus and MEDLINE.

Late oxidation of hexose based building blocks or the use of uronic acid containing building blocks are two complementary strategies in the synthesis of glycosaminoglycans. Here we report the synthesis and evaluation of various disaccharide donors-uronic acids and their pyranose equivalent-for the synthesis of heparan sulfate, using an established protective group strategy. Hexose based “imidate” type donors perform well in the studied glycosylation, while their corresponding uronate esters fall short; a uronate ester thioglycoside performs equal to, if not better than, a hexose thioglycoside equivalent

Organic & Biomolecular 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 C4H4N2O2, HPLC of Formula: 4972-31-0.

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

Ribeiro da Silva, Manuel A. V. published the artcileExperimental Study on the Thermochemistry of Some Derivatives of Piperidinol, Application of 1-Ethylpiperidin-3-ol, the publication is Journal of Chemical & Engineering Data (2006), 51(2), 767-771, database is CAplus.

Standard (p° = 0.1 MPa) energies of combustion for 1-methyl-3-piperidinol, 1-ethyl-3-piperidinol, and 1-methyl-4-piperidinol were measured at 298.15 K by static bomb calorimetry. The standard molar enthalpies of formation of the condensed phase were derived. The standard molar enthalpies of vaporization at 298.15 K of the three piperidinol derivatives studied were determined by high-temperature Calvet microcalorimetry. The resp. standard molar enthalpies of formation in the gaseous phase at 298.15 K were derived.

Journal of Chemical & Engineering Data published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C7H15NO, Application of 1-Ethylpiperidin-3-ol.

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

Hong, Misun published the artcileSinglet Oxygen in Lithium-Oxygen Batteries, Related Products of piperidines, the publication is Batteries & Supercaps (2021), 4(2), 286-293, database is CAplus.

A review. Singlet oxygen (¹O₂) is one of the most critical species leading to parasitic side reactions and poor reversibility in non-aqueous Li-O₂ batteries. ¹O₂ is generated via the disproportionation of the superoxide radical (O₂.-) in O₂/Li₂O₂ electrochem. The mechanistic and computational studies on ¹O₂ formation revealed the significant roles of the associated cations, solvation ability of aprotic solvents, H⁺ source, and catalyst/electrode materials. Along with efforts to alleviate ¹O₂ production, trapping and eliminating ¹O₂ have been attempted using mol. agents. Anthracene derivatives trap ¹O₂ and form endoperoxides, which can be quant. detected using in situ fluorescence anal. Phys. quenchers that convert ¹O₂ to ³O₂ are desirable for cycling of Li-O₂ cells because quencher mols. are reusable. We highlight the recent reports on the formation and elimination of ¹O₂, and challenges and perspectives of suppressing the ¹O₂ effect on the performance of Li-O₂ cells.

Batteries & Supercaps 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, Related Products of piperidines.

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

Kosak, Urban published the artcileStraightforward synthesis of orthogonally protected piperidin-3-ylmethanamine and piperidin-4-ylmethanamine derivatives, Related Products of piperidines, the publication is Tetrahedron Letters (2014), 55(12), 2037-2039, database is CAplus.

The synthesis of orthogonally protected piperidin-3-ylmethanamines and piperidin-4-ylmethanamines from com. available nipecotamide, isonipecotamide, nipecotic acid, and isonipecotic acid was presented. This is a straightforward 2-step procedure that gives high overall yields. Purification of the intermediates is not necessary, and the final compounds are purified by simple flash column chromatog.

Tetrahedron Letters published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Related Products of piperidines.

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

Kosak, Urban published the artcileThe Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity, HPLC of Formula: 39546-32-2, the publication is Journal of Medicinal Chemistry (2018), 61(1), 119-139, database is CAplus and MEDLINE.

The enzymic activity of butyrylcholinesterase (BChE) in the brain increases with the progression of Alzheimer’s disease, thus classifying BChE as a promising drug target in advanced Alzheimer’s disease. Structure-based drug discovery approaches to develop potent, selective and reversible human BChE inhibitors was used. The most potent, compound I, had a picomolar inhibition constant vs. BChE due to strong cation-π interactions, as revealed by the solved crystal structure of its complex with human BChE. Addnl., compound I inhibits BChE ex vivo and is noncytotoxic. In vitro pharmacokinetic experiments show that compound I is highly protein bound, highly permeable and metabolically stable. Finally, compound I crosses the blood-brain barrier, and it improves memory, cognitive functions and learning abilities of mice in a scopolamine model of dementia. Compound I is thus a promising advanced lead compound for the development of drugs for alleviating symptoms of cholinergic hypofunction in patients with advanced Alzheimer’s disease.

Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, HPLC of Formula: 39546-32-2.

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

Kosak, Urban published the artcileDevelopment of an in-vivo active reversible butyrylcholinesterase inhibitor, HPLC of Formula: 39546-32-2, the publication is Scientific Reports (2016), 39495, database is CAplus and MEDLINE.

Alzheimer’s disease (AD) is characterized by severe basal forebrain cholinergic deficit, which results in progressive and chronic deterioration of memory and cognitive functions. Similar to acetylcholinesterase, butyrylcholinesterase (BChE) contributes to the termination of cholinergic neurotransmission. Its enzymic activity increases with the disease progression, thus classifying BChE as a viable therapeutic target in advanced AD. Potent, selective and reversible human BChE inhibitors were developed. The solved crystal structure of human BChE in complex with the most potent inhibitor reveals its binding mode and provides the mol. basis of its low nanomolar potency. Addnl., this compound is noncytotoxic and has neuroprotective properties. Furthermore, this inhibitor moderately crosses the blood-brain barrier and improves memory, cognitive functions and learning abilities of mice in a model of the cholinergic deficit that characterizes AD, without producing acute cholinergic adverse effects. Our study provides an advanced lead compound for developing drugs for alleviating symptoms caused by cholinergic hypofunction in advanced AD.

Scientific Reports published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, HPLC of Formula: 39546-32-2.

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

Bellomo, Piero published the artcileSynthesis and antibacterial activity of some derivatives of tolypomycinone. Relation between structure and activity in ansamycins, COA of Formula: C7H16N2, the publication is Journal of Medicinal Chemistry (1977), 20(10), 1287-91, database is CAplus and MEDLINE.

A series of 29 3-aminotolypomycinone derivatives and 3,16-diamino-16,17-dihydrotolypomycinone derivatives were prepared by addition of a primary or secondary amine to tolypomycinone, and 3-(methylamino)-16,17-dihydrotolypomycinone was prepared by addition of MeNH₂ to 16,17-dihydrotolypomycinone. One of the most active compounds, 3-[2-(N-morpholyl)ethylamino]tolypomycinone (I), had enhanced stability and prolonged activity against Staphylococcus aureus in acid and alk. solutions as compared to tolypomycin Y. In vitro tests showed high antibacterial activity for several compounds against S. aureus and 3 strains of gram-neg. bacteria. Structure-activity relations are discussed.

Journal of Medicinal Chemistry published new progress about 14613-37-7. 14613-37-7 belongs to piperidines, auxiliary class Piperidine,Amine, name is (1-Methylpiperidin-3-yl)methanamine, and the molecular formula is C7H16N2, COA of Formula: C7H16N2.

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

Leadbetter, Elizabeth A. published the artcileNK T cells provide lipid antigen-specific cognate help for B cells, COA of Formula: C11H15NOS, the publication is Proceedings of the National Academy of Sciences of the United States of America (2008), 105(24), 8339-8344, database is CAplus and MEDLINE.

The mechanisms of T cell help for production of antilipid antibodies are largely unknown. This study shows that invariant NK T cells (iNK T cells) and B cells cooperate in a model of antilipid antigen-specific antibody responses. We use a model haptenated lipid mol., 4-hydroxy-3-nitrophenyl-αGalactosylCeramide (NP-αGalCer), to demonstrate that iNK T cells provide cognate help to lipid-antigen-presenting B cells. B cells proliferate and IgG anti-NP is produced from in vivo-immunized mice and in vitro cocultures of B and NK T cells after exposure to NP-αGalCer, but not closely related control glycolipids. This B cell response is absent in CD1d^-/- and Jα18^-/- mice but not CD4^-/- mice. The antibody response to NP-αGalCer is dominated by the IgM, IgG3, and IgG2c isotypes, and marginal zone B cells stimulate better in vitro lipid antigen-driven proliferation than follicular B cells, suggesting an important role for this B cell subset. iNK T cell help for B cells is shown to involve cognate help from CD1d-instructed lipid-specific iNK T cells, with help provided via CD40L, B7-1/B7-2, and IFN-γ, but not IL-4. This model provides evidence of iNK T cell help for antilipid antibody production, an important aspect of infections, autoimmune diseases, and vaccine development. Our findings also now allow prediction of those microbial antigens that would be expected to elicit cognate iNKT cell help for antibody production, namely those that can stimulate iNKT cells and at the same time have a polar moiety that can be recognized by antibodies.

Proceedings of the National Academy of Sciences of the United States of America 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

Gordon, Richard K. published the artcileDistance geometry of α-substituted 2,2-diphenylpropionate antimuscarinics, SDS of cas: 13444-24-1, the publication is Molecular Pharmacology (1989), 36(5), 766-72, database is CAplus and MEDLINE.

Quant. relationships between pharmacol. activities and phys. properties of a series of 2,2-diphenylpropionate compounds were used to define the topog. of the antagonist binding site of muscarinic receptors. XICAMM, a computer mol. modeling program, was used to calculate geometric and topol. values of the compounds The compounds were tested for their antimuscarinic activities by inhibition of [N-methyl-³H]scopolamine binding to the muscarinic receptors of N4TG1 neuroblastoma cells, by inhibition of carbachol-induced α-amylase release from rat pancreas acini, and by blocking acetylcholine-induced contraction of guinea pig ileum. To evaluate only the effect of the bond distance on the potency of the synthesized antimuscarinics, the compounds were designed to contain as many constant features as possible. Neither the hydrophobic nor the ester moieties of the compounds were changed, and the rings containing the protonated N saturated and restricted. The antimuscarinic activities obtained from the 3 assays correlated with each other, with the exception of 2 compounds The 2 compounds demonstrated specificity for the M3 muscarinic receptor subtype in the pancreas. The antimuscarinic activities were related to the bond distances between the carbonyl O (constant electroneg. locus) and the protonated N (center of cationic charge) of the 2,2-diphenylpropionate compounds Parabolic relationships between the pharmacol. activities and bond distances were empirically established. The shortest calculated bond distance of these compounds was ∼4.4 Å, whereas the longest was ∼5.9 Å. The maximum antimuscarinic potency was observed with a calculated bond distance of ∼5.2 Å in all 3 assays.

Molecular Pharmacology published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C7H15NO, SDS of cas: 13444-24-1.

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

Bataille, Carole J. R. published the artcileThiazolidine derivatives as potent and selective inhibitors of the PIM kinase family, Synthetic Route of 634905-21-8, the publication is Bioorganic & Medicinal Chemistry (2017), 25(9), 2657-2665, database is CAplus and MEDLINE.

The PIM family of serine/threonine kinases have become an attractive target for anti-cancer drug development, particularly for certain hematol. malignancies. Here, we describe the discovery of a series of inhibitors of the PIM kinase family using a high throughput screening strategy. Through a combination of mol. modeling and optimization studies, the intrinsic potencies and mol. properties of this series of compounds was significantly improved. An excellent pan-PIM isoform inhibition profile was observed across the series, while optimized examples show good selectivity over other kinases. Two PIM-expressing leukemic cancer cell lines, MV4-11 and K562, were employed to evaluate the in vitro anti-proliferative effects of selected inhibitors. Encouraging activities were observed for many examples, with the best example (44) giving an IC₅₀ of 0.75 μM against the K562 cell line. These data provide a promising starting point for further development of this series as a new cancer therapy through PIM kinase inhibition.

Bioorganic & Medicinal Chemistry published new progress about 634905-21-8. 634905-21-8 belongs to piperidines, auxiliary class Piperidine,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (3-(Piperidin-1-yl)phenyl)boronic acid, and the molecular formula is C11H16BNO2, Synthetic Route of 634905-21-8.

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