Month: December 2022

Song, Mingxia published the artcileDesign, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H₃ receptor antagonists/inverse agonists containing triazole moiety, Quality Control of 39546-32-2, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2020), 35(1), 1310-1321, database is CAplus and MEDLINE.

Histamine H₃ receptors (H₃R) antagonists/inverse agonists are becoming a promising therapeutic approach for epilepsy. In this article, novel nonimidazole H₃R antagonists/inverse agonists have been designed and synthesized via hybriding the H₃R pharmacophore (aliphatic amine with propyloxy chain) with the 1,2,4-triazole moiety as anticonvulsant drugs. The majority of antagonists/inverse agonists prepared here exerted moderate to robust activities in cAMP-response element (CRE) luciferase screening assay. 1-(3-(4-(3-Phenyl-4H-1,2,4-triazol-4-yl)phenoxy)propyl)piperidine () and 1-(3-(4-(3-(4-chlorophenyl)-4H-1,2,4-triazol-4-yl)phenoxy)propyl)piperidine displayed the highest H₃R antagonistic activities, with IC₅₀ values of 7.81 and 5.92 nM, resp. Meanwhile, the compounds with higher H₃R antagonistic activities exhibited protection for mice in maximal electroshock seizure (MES)-induced convulsant model. Moreover, the protection of against the MES induced seizures was fully abrogated when mice were co-treated with RAMH, a CNS-penetrant H₃R agonist, which suggested that the potential therapeutic effect of was through H₃R. These results indicate that the attempt to find new anticonvulsant among H₃R antagonists/inverse agonists is practicable.

Journal of Enzyme Inhibition and 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 C12H17NS2, Quality Control of 39546-32-2.

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

Teramoto, Hiroyoshi published the artcileDesign and synthesis of a piperidinone scaffold as an analgesic through kappa-opioid receptor: Structure-activity relationship study of matrine alkaloids, Recommanded Product: Piperidine-4-carboxamide, the publication is Chemical & Pharmaceutical Bulletin (2016), 64(5), 410-419, database is CAplus and MEDLINE.

The matrine-type alkaloid 4-dimethylamino-1-pentanoylpiperidine (I) has an antinociceptive effect through its impact on the κ-opioid receptor (KOR). Derivatives of I were synthesized by altering its amide and tertiary amine groups; and they were evaluated for their antinociceptive effects. The results indicated that the distance between these groups on I was optimal for the antinociceptive effect. The effects obtained with racemic compounds II [R = β-CH₂Ph, α-CH₂Ph, R¹ = α-H, R² = R³ = H; R = β-CH₂Ph, α-CH₂Ph, R¹ = α-H, R² = (CH₂)₄Me, R³ = H; R = H, R¹ = α-H, β-H, R² = H, R³ = β-CH₂Ph; R = H, R¹ = α-H, β-H, R² = (CH₂)₄Me, R³ = β-CH₂Ph] and (-)-II [R = β-CH₂Ph, R¹ = β-H, R² = H, (CH₂)₄Me, R³ = H] indicated that the relative configuration of the 3- and 4-substituents influenced the effect mediated through the KOR.

Chemical & Pharmaceutical Bulletin 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 C18H28B2O4, Recommanded Product: Piperidine-4-carboxamide.

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

Kimura, Yasuaki published the artcileDesign and synthesis of immobilized Tamiflu analog on resin for affinity chromatography, SDS of cas: 35661-58-6, the publication is Tetrahedron Letters (2009), 50(26), 3205-3208, database is CAplus.

A resin linked with the Tamiflu core was synthesized by modifying the original synthetic route of oseltamivir phosphate (Tamiflu). The prepared resin bound to the influenza virus enzyme neuraminidase, the main target of Tamiflu. The immobilized Tamiflu analog will be useful for isolating and identifying presumed endogenous vertebrate proteins that interact with Tamiflu, which might relate to the abnormal behavior exhibited by some influenza patients treated with Tamiflu.

Tetrahedron Letters published new progress about 35661-58-6. 35661-58-6 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-((9H-Fluoren-9-yl)methyl)piperidine, and the molecular formula is C19H21N, SDS of cas: 35661-58-6.

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

Sawai, Yasuhiro published the artcileProcess for the Preparation of an Amorphous, Peptide-like Diabetes Drug: Approach to a Chromatography-Free Process, Category: piperidines, the publication is Organic Process Research & Development (2010), 14(5), 1110-1117, database is CAplus.

A manufacturing process suitable for large-scale production of the peptide-like amorphous compound N-((2R)-1-{(3R)-6-chloro-3-[(dimethylamino)methyl]-3,4-dihydroquinolin-1(2H)-yl}-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-1-[(1-methyl-1H-indol-2-yl)carbonyl]piperidine-4-carboxamide (I) as a drug for treating diabetes has been developed. The first kilogram quantities of I were prepared via a single-chromatog. process that employed recyclable cation-exchange resin chromatog. for an amorphous intermediate (2R)-2-amino-1-[(3R)-6-chloro-3-[(dimethylamino)methyl]-3,4-dihydroquinolin-1(2H)-yl]-3-(1H-indol-3-yl)-propan-1-one (II). We have also developed a chromatog.-free process that involves a combination purification of extraction of II with crystallization of II·0.25H₃PO₄·0.5H₂O. The latter process afforded amorphous compound I with >98% purity by HPLC area anal., the same quality as that provided by the former process.

Organic Process Research & Development published new progress about 35661-58-6. 35661-58-6 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-((9H-Fluoren-9-yl)methyl)piperidine, and the molecular formula is C19H21N, Category: piperidines.

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

Yamago, Shigeru published the artcileIterative glycosylation of 2-deoxy-2-aminothioglycosides and its application to the combinatorial synthesis of linear oligo-glucosamines, Application of 1-(Phenylsulfinyl)piperidine, the publication is Angewandte Chemie, International Edition (2004), 43(16), 2145-2148, database is CAplus and MEDLINE.

Highly efficient coupling is observed with thioglycosides, which act both as glycosyl donors and acceptors. The iteration of the glycoside-coupling reaction under the same conditions allows the rapid assembly of a library of linear oligo-glucosamines (Phth = phthaloyl).

Angewandte Chemie, International Edition 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 C3H5BN2O2, Application of 1-(Phenylsulfinyl)piperidine.

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

Chowdhury, Firoz Alam published the artcileCO₂ Capture by Tertiary Amine Absorbents: A Performance Comparison Study, Safety of 1-Ethylpiperidin-3-ol, the publication is Industrial & Engineering Chemistry Research (2013), 52(24), 8323-8331, database is CAplus.

This work assessed CO₂ capture with 24 tertiary amine absorbents (including 3 synthetic amines) with systematic modification of their chem. structures. Aqueous amine solutions (30 % mass fraction) were used to evaluate CO₂ capture performance. Laboratory gas scrubbing, vapor-liquid equilibrium, and reaction calorimetry experiments were conducted to obtain the absorption rate, amount of CO₂ absorbed, cyclic CO₂ capacity, and heat of reaction for each absorbent. Results for were compared with the conventional tertiary absorbent, N-methyldiethanolamine (MDEA). Seven of the studied absorbents performed well with high absorption rates and cyclic capacities. Among these absorbents, some displayed lower heats of reaction than MDEA. Results provided basic guidelines to discover potential tertiary amine-based absorbents which may lead to development of new absorbent systems for CO₂ capture.

Industrial & Engineering Chemistry Research 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, Safety of 1-Ethylpiperidin-3-ol.

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

Mavunkel, Babu published the artcilePyrimidine-based inhibitors of CaMKIIδ, Formula: C11H16BNO2, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(7), 2404-2408, database is CAplus and MEDLINE.

Non-ATP competitive pyrimidine-based inhibitors of CaMKIIδ were identified. Computational studies were enlisted to predict the probable mode of binding. The results of the computational studies led to the design of ATP competitive inhibitors with optimized hinge interactions. Inhibitors of this class possessed improved enzyme and cellular activity compared to early leads.

Bioorganic & Medicinal Chemistry Letters 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, Formula: C11H16BNO2.

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

Zhang, Hua published the artcileQuantification and molecular imaging of fatty acid isomers from complex biological samples by mass spectrometry, COA of Formula: C20H22ClN3O3, the publication is Chemical Science (2021), 12(23), 8115-8122, database is CAplus and MEDLINE.

Elucidating the isomeric structure of free fatty acids (FAs) in biol. samples is essential to comprehend their biol. functions in various physiol. and pathol. processes. Herein, we report a novel approach of using peracetic acid (PAA) induced epoxidation coupled with mass spectrometry (MS) for localization of the C-C bond in unsaturated FAs, which enables both quantification and spatial visualization of FA isomers from biol. samples. Abundant diagnostic fragment ions indicative of the C-C positions were produced upon fragmentation of the FA epoxides derived from either in-solution or on-tissue PAA epoxidation of free FAs. The performance of the proposed approach was evaluated by anal. of FAs in human cell lines as well as mapping the FA isomers from cancer tissue samples with MALDI-TOF/TOF-MS. Merits of the newly developed method include high sensitivity, simplicity, high reaction efficiency, and capability of spatial characterization of FA isomers in tissue samples.

Chemical Science published new progress about 1032229-33-6. 1032229-33-6 belongs to piperidines, auxiliary class Metabolic Enzyme,SCD, name is 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide, and the molecular formula is C9H21NO3, COA of Formula: C20H22ClN3O3.

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

Crich, David published the artcileDirect Stereocontrolled Synthesis of 3-Amino-3-deoxy-β-Mannopyranosides: Importance of the Nitrogen Protecting Group on Stereoselectivity, Safety of 1-(Phenylsulfinyl)piperidine, the publication is Journal of Organic Chemistry (2007), 72(14), 5183-5192, database is CAplus and MEDLINE.

The highly stereocontrolled synthesis of the 3-amino-3-deoxy-β-mannopyranosides is achieved by means of thioglycoside donors protected with a 4,6-O-benzylidene or alkylidene acetal and a benzylidene imine group. Among the various nitrogen protecting groups investigated only the Schiff’s base was found to give high β-selectivity. N-Phthalimido and N-acetamido protected donors were found to be highly α-selective, whereas 3-azido-3-deoxy glycosyl donors gave intermediate selectivity. The reasons for the protecting group dependency are discussed in terms of the change in the O2-C₂-C₃-N3 torsional interaction on conversion of the covalent glycosyl triflates to the transient oxa-carbenium ions.

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, Safety of 1-(Phenylsulfinyl)piperidine.

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

Xi, Xiaomin published the artcileIncreased Varietal Aroma Diversity of Marselan Wine by Mixed Fermentation with Indigenous Non-Saccharomyces Yeasts, SDS of cas: 826-36-8, the publication is Fermentation (2021), 7(3), 133, database is CAplus.

The common use of com. yeasts usually leads to dull wine with similar aromas and tastes. Therefore, screening for novel indigenous yeasts to practice is a promising method. In this research, aroma discrepancies among six wine groups fermentated with indigenous yeasts were analyzed. Three Saccharomyces yeasts (FS36, HL12, YT28) and three matched non-Saccharomyces yeasts (FS31, HL9, YT2) were selected from typical Chinese vineyards. The basic oenol. parameters, aroma compounds, and sensory evaluation were analyzed. The results showed that each indigenous Saccharomyces yeast had excellent fermentation capacity, and mixed-strain fermentation groups produced more glycerol, contributing to sweeter and rounder taste. The results from GC-MS, principal components anal. (PCA), and sensory evaluation highlighted that the HL mixed group kept the most content of Marselan varietal flavors such as calamenene and β-damascone hereby ameliorated the whole aroma quality. Our study also implied that the indigenous yeast from the same region as the grape variety seems more conducive to preserve the natural variety characteristics of grapes.

Fermentation 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 C7H13NO2, SDS of cas: 826-36-8.

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