Category: piperidines

Related Products of 38092-89-6, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 38092-89-6, Name is 8-Chloroazatadine, SMILES is CN1CC/C(CC1)=C2C3=CC=C(Cl)C=C3CCC4=CC=CN=C42, belongs to piperidines compound. In a article, author is Lee, Na-Ra, introduce new discover of the category.

New Scaffold for Lead Compounds to Treat Methamphetamine Use Disorders

Despite increased methamphetamine use worldwide, pharmacotherapies are not available to treat methamphetamine use disorder. The vesicular monoamine transporter-2 (VMAT2) is an important pharmacological target for discovery of treatments for methamphetamine use disorder. VMAT2 inhibition by the natural product, lobeline, reduced methamphetamine-evoked dopamine release, methamphetamine-induced hyperlocomotion, and methamphetamine self-administration in rats. Compared to lobeline, lobelane exhibited improved affinity and selectivity for VMAT2 over nicotinic acetylcholine receptors. Lobelane inhibited neurochemical and behavioral effects of methamphetamine, but tolerance developed to its behavioral efficacy in reducing methamphetamine self-administration, preventing further development. The lobelane analog, R-N-(1,2-dihydroxypropyl)-2,6-cis-di(4-methoxyphenethyl) piperidine hydrochloride (GZ-793A), potently and selectively inhibited VMAT2 function and reduced neurochemical and behavioral effects of methamphetamine. However, GZ-793A exhibited potential to induce ventricular arrhythmias interacting with human-ether-a-go-go (hERG) channels. Herein, a new lead, R-3-(4-methoxyphenyl)- N-(1-phenylpropan-2-yl) propan-1-amine (GZ-11610), from the novel scaffold (N-alkyl(1-methyl-2-phenylethyl) amine) was evaluated as a VMAT2 inhibitor and potential therapeutic for methamphetamine use disorder. GZ-11610 was 290-fold selective for VMAT2 over dopamine transporters, suggesting that it may lack abuse liability. GZ-11610 was 640-to 3500-fold selective for VMAT2 over serotonin transporters and nicotinic acetylcholine receptors. GZ-11610 exhibited > 1000-fold selectivity for VMAT2 over hERG, representing a robust improvement relative to our previous VMAT2 inhibitors. GZ-11610 (330 mg/kg, s.c. or 56-300 mg/kg, oral) reduced methamphetamine-induced hyperactivity in methamphetamine-sensitized rats. Thus, GZ-11610 is a potent and selective inhibitor of VMAT2, may have low abuse liability and low cardiotoxicity, and after oral administration is effective and specific in inhibiting the locomotor stimulant effects of methamphetamine, suggesting further investigation as a potential therapeutic for methamphetamine use disorder.

Related Products of 38092-89-6, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 38092-89-6 is helpful to your research.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, 10465-81-3, Name is Diazene-1,2-diylbis(piperidin-1-ylmethanone), SMILES is O=C(/N=N/C(N1CCCCC1)=O)N2CCCCC2, belongs to piperidines compound. In a document, author is Tikhov, Rabdan M., introduce the new discover, Safety of Diazene-1,2-diylbis(piperidin-1-ylmethanone).

Construction of piperidine-2,4-dione-type azaheterocycles and their application in modern drug development and natural product synthesis

The current review summarizes the latest achievements in the synthesis of piperidine-2,4-dione-type azaheterocycles. Two main groups traditional (carbonyl compound transformations) and novel (anionic enolate rearrangements) of complementary methods for the simple and effective preparation of structurally diverse compounds in racemic and enantiopure forms have been reported. Due to the specific structure and appropriate reactivity profiles of dione-type molecules, they are a convenient modern platform for the construction of functionalized piperidine-type systems possessing high synthetic and medicinal potential. This potential is successfully realized by the creation of highly active pharmaceutically relevant compounds and the synthesis of natural products.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 10465-81-3 is helpful to your research. Safety of Diazene-1,2-diylbis(piperidin-1-ylmethanone).

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Application of 4005-49-6, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 4005-49-6, Name is N-(7H-Purin-6-yl)benzamide, SMILES is O=C(NC1=C2NC=NC2=NC=N1)C3=CC=CC=C3, belongs to piperidines compound. In a article, author is Li, Hui, introduce new discover of the category.

Antidiabetic compounds 8a, 8b, 8k, and 9h enhance insulin secretion: activity and mechanism

Purpose This study primarily investigated the effects of hypoglycemic compounds (Imeglimin derivatives) on insulin secretion in type 2 diabetes mellitus (T2DM), and further explored the possible mechanism underlying these effects. Methods Firstly, Metformin was used as the initiating compound to synthesize three sets of derivatives which contained Imeglimin structure core. At the cellular level, we screened compounds with better effect on the activity of insulin receptor tyrosine protein kinase (IFcTPK) after the islet beta cells were treated with the compounds of different concentrations. The insulin secretion was assessed using radioimmunoassay and the cytotoxicity to islet beta cells was evaluated by means of MTT assay following treatment with the compounds. The Ca2+-related mechanism by which these compounds promote insulin secretion was elucidated with whole cell recordings from current-clamp mode. Results Totally, 48 synthesized compounds were generated, wherein 10 compounds could increase the activity of IFcTPK in HIT-T15 cells better among these compounds. The modified Imeglimin, especially in the structure of hydrophilic hydroxyl or piperidine rings, could improve the activity of the compound to promote insulin secretion. Furthermore, the compounds 8a, 8b, 8k, and 9h revealed high insulin secretion-promoting activity. These compounds enhanced insulin secretion in islet beta cells by repressing the ATP-sensitive K(+) and voltage-gated K+ pathway. Conclusions Our findings indicate that the hypoglycemic compounds 8a, 8b, 8k, and 9h confer better promotive effect on insulin secretion, which provides a reference for the development of drugs with better hypoglycemic activity.

Application of 4005-49-6, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 4005-49-6 is helpful to your research.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 14047-28-0, Name is (R)-1-(6-Amino-9H-purin-9-yl)propan-2-ol, molecular formula is C8H11N5O, belongs to piperidines compound, is a common compound. In a patnet, author is Petchey, Mark R., once mentioned the new application about 14047-28-0, Formula: C8H11N5O.

Biocatalytic Synthesis of Moclobemide Using the Amide Bond Synthetase McbA Coupled with an ATP Recycling System

The biocatalytic synthesis of amides from carboxylic acids and primary amines in aqueous media can be achieved using the ATP-dependent amide bond synthetase McbA, via an adenylate intermediate, using only 1.5 equiv of the amine nucleophile. Following earlier studies that characterized the broad carboxylic acid specificity of McbA, we now show that, in addition to the natural amine substrate 2-phenylethylamine, a range of simple aliphatic amines, including methylamine, butylamine, and hexylamine, and propargylamine are coupled efficiently to the native carboxylic acid substrate 1-acetyl-9H-beta-carboline-3-carboxylic acid by the enzyme, to give amide products with up to >99% conversion. The structure of wild-type McbA in its amidation conformation, coupled with modeling and mutational studies, reveal an amine access tunnel and a possible role for residue D201 in amine activation. Amide couplings were slower with anilines and alicyclic secondary amines such as pyrrolidine and piperidine. The broader substrate specificity of McbA was exploited in the synthesis of the monoamine oxidase A inhibitor moclobemide, through the reaction of 4-chlorobenzoic acid with 1.5 equiv of 4-(2-aminoethyl)morpholine, and utilizing polyphosphate kinases SmPPK and AjPPK in the presence of polyphosphoric acid and 0.1 equiv of ATP, required for recycling of the cofactor.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 14047-28-0. The above is the message from the blog manager. Formula: C8H11N5O.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 34737-89-8, Name is 1-Benzyl-3-methylpiperidin-4-one, SMILES is O=C1C(C)CN(CC2=CC=CC=C2)CC1, belongs to piperidines compound. In a document, author is Namera, Dipti L., introduce the new discover, HPLC of Formula: C13H17NO.

Arylidene analogues as selective COX-2 inhibitors: synthesis, characterization,in silicoandin vitrostudies

Pyrazole derivatives are known to be as non-steroidal anti-inflammatory drugs (NSAID).Celecoxibis the pioneer sulfonamide being pyrazole derivative COX-2 inhibitors, which used to treat pain and inflammation; they may also have a role in cancer prevention. In the present investigation, a series of arylidene analogues (NDP-4011toNDP-4016) were synthesized by the condensation of 4-(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl) benzenesulfonamide (I) with various substituted aromatic aldehydes in ethanol using a catalytic amount of piperidine. All the synthesized compounds were well characterized by IR,H-1 NMR,C-13 NMR and mass spectrometry. The cytotoxicity of synthesized compounds was tested on theNRK-52Ecell line. From whichNDP-4011,NDP-4012,NDP-4013,NDP-1015andNDP-4016were found to have higher cytotoxicity whereasNDP-4014showed less cytotoxicity compared toCelecoxib. Thein silicopharmacokinetic parameters of compounds were evaluated to check their candidature as a drug. Molecular docking was carried out on COX-2 structures, which revealed thatNDP-4011toNDP-4016targets allosteric binding site similar to the binding mode of the selective COX inhibitorCelecoxib. Furthermore, results ofin vitroCOX-2 inhibition assay supports arylidene analogues as COX-2 inhibitors.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 34737-89-8 is helpful to your research. HPLC of Formula: C13H17NO.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

In an article, author is Roque, Jose B., once mentioned the application of 41556-26-7, Formula: C30H56N2O4, Name is Bis(1,2,2,6,6-pentamethylpiperidin-4-yl) decanedioate, molecular formula is C30H56N2O4, molecular weight is 508.78, MDL number is MFCD00134706, category is piperidines. Now introduce a scientific discovery about this category.

Deconstructive fluorination of cyclic amines by carbon-carbon cleavage

Deconstructive functionalizations involving scission of carbon-carbon double bonds are well established. In contrast, unstrained C(sp(3))-C(sp(3)) bond cleavage and functionalization have less precedent. Here we report the use of deconstructive fluorination to access mono-and difluorinated amine derivatives by C(sp(3))-C(sp(3)) bond cleavage in saturated nitrogen heterocycles such as piperidines and pyrrolidines. Silver-mediated ring-opening fluorination using Selectfluor highlights a strategy for cyclic amine functionalization and late-stage skeletal diversification, establishing cyclic amines as synthons for amino alkyl radicals and providing synthetic routes to valuable building blocks.

If you are interested in 41556-26-7, you can contact me at any time and look forward to more communication. Formula: C30H56N2O4.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 179474-79-4, Name is 1-(3-Methoxypropyl)piperidin-4-amine, molecular formula is C9H20N2O. In an article, author is Zhi, Zhuoer,once mentioned of 179474-79-4, COA of Formula: C9H20N2O.

Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors

Most of the current monoacylglycerol lipase (MAGL) inhibitors function by an irreversible mechanism of action, causing a series of side effects. Herein, starting from irreversible inhibitors, 25 compounds were synthesized and evaluated in vitro for MAGL inhibition, among which, compound 36 showed the most potent inhibitory activity (IC50 = 15 nM). Crucially, docking studies demonstrated that the m-chlorine-substituted aniline fragment occupied a hydrophobic subpocket enclosed by side chains of Val191, Tyr194, Val270, and Lys273, which creatively identify a new key anchoring point for the development of new MAGL inhibitors. Furthermore, in vivo evaluation innovatively revealed that this reversible inhibitor 36 significantly ameliorated depressive-like behaviors induced by reserpine. To the best of our knowledge, this is the first time that reversible inhibitors of MAGL were developed to support MAGL as a potential therapeutic target for depression.

Interested yet? Keep reading other articles of 179474-79-4, you can contact me at any time and look forward to more communication. COA of Formula: C9H20N2O.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 120-73-0, Name is Purine, molecular formula is C5H4N4. In an article, author is Antermite, Daniele,once mentioned of 120-73-0, Application In Synthesis of Purine.

Regio- and Stereoselective Palladium-Catalyzed C(sp(3))-H Arylation of Pyrrolidines and Piperidines with C(3) Directing Groups

The selective synthesis of cis-3,4-disubstituted pyrrolidines and piperidines is achieved by a Pd-catalyzed C-H arylation with excellent regio- and stereoselectivity using an aminoquinoline auxiliary at C(3). The arylation conditions are silver free, use a low catalyst loading, and employ inexpensive K2CO3 as a base. Directing group removal is accomplished under new, mild conditions to access amide-, acid-, ester-, and alcohol-containing fragments and building blocks. This C-H arylation protocol enabled a short and stereocontrolled formal synthesis of (-)-paroxetine.

If you¡¯re interested in learning more about 120-73-0. The above is the message from the blog manager. Application In Synthesis of Purine.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 201341-05-1, Name is Tenofovir disoproxil, SMILES is O=C(OC(C)C)OCOP(OCOC(OC(C)C)=O)(CO[C@H](C)CN1C=NC2=C(N)N=CN=C12)=O, belongs to piperidines compound. In a document, author is Song, Cheng, introduce the new discover, Category: piperidines.

Metabolomics analysis of nitrogen-containing metabolites between two Dendrobium plants

Nitrogen-containing compounds especially alkaloids are important medicinal ingredients in caulis dendrobii plants. Using solid-phase extraction coupled with liquid chromatography tandem mass spectrometry and multivariate data analysis methods, metabolic profiling of the nitrogen-containing compounds was established to distinguish Dendrobium huoshanense and Dendrobium officinale. Hundreds of nitrogen-containing compounds from the two caulis dendrobii were purified by the MCX cartridges. Some compounds were identified by high-resolution tandem mass spectrometry technology. Together with multivariate data analysis methods, comparative analysis of the metabolic profiling from two caulis dendrobii was conducted. A total of 133 nitrogen-containing compounds were identified, including amino acids, pyrrolidines, tropanes, pyrimidines, purines, indoles, piperidines, guanidines, quinolines, isoquinolines and terpenoids. Metabolic profiling analysis showed that the composition and contents of these chemical components were significantly different between D. huoshanense and D. officinale. Moreover, some components were species-specific, distributed in the two caulis dendrobii, such as pilosine, ternatusine, etc. Because alkaloids are mainly derived from amino acids via multistep biochemical reactions, the correlation analysis suggested that amino acids were partially associated with several types of components and significantly correlated with certain alkaloids. Arginine was extremely correlated with guanidines. Pyrimidines, purines and niacin-nicotinamide metabolic intermediates were associated with three independent networks. The results further enriched the chemical components currently identified from caulis dendrobii and provided a technical reference for detecting nitrogen-containing compounds in other medicinal plants.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 201341-05-1 is helpful to your research. Category: piperidines.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Synthetic Route of 827026-45-9, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 827026-45-9, Name is 3-(4-Nitro-1-oxoisoindolin-2-yl)piperidine-2,6-dione, SMILES is [O-][N+](=O)C1=C2CN(C3CCC(=O)NC3=O)C(=O)C2=CC=C1, belongs to piperidines compound. In a article, author is Wakiyama, Yoshinari, introduce new discover of the category.

Synthesis and SARs of novel lincomycin derivatives Part 5: optimization of lincomycin analogs exhibiting potent antibacterial activities by chemical modification at the 6-and 7-positions

In order to modify lincomycin at the C-6 and C-7 positions, we prepared target molecules, which have substituted pipecolinic acid at the 6-amino group and a para-substituted phenylthio group at the C-7 position, in application of palladium-catalyzed cross-coupling as a key reaction. As the result of structure-activity relationship (SAR) studies at the 6-position, analogs possessing 4′-cis-(cyclopropylmethyl) piperidine showed significantly strong antibacterial activities against Streptococcus pneumoniae and Streptococcus pyogenes with an erm gene. On the basis of SAR, we further synthesized novel analogs possessing 4′-cis-(cyclopropylmethyl) piperidine by transformation of a C-7 substituent. Consequently, novel derivatives possessing a paraheteroaromatic-phenylthio group at the C-7 position exhibited significantly strong activities against S. pneumoniae and S. pyogenes with an erm gene even when compared with those of telithromycin. Finally, in vivo efficacy of selected two derivatives was evaluated in a rat pulmonary infection model with resistant S. pneumoniae with erm + mef genes. One of them exhibited strong and constant in vivo efficacy in this model, and both compounds showed strong in vivo efficacy against resistant S. pneumoniae with a mef gene.

Synthetic Route of 827026-45-9, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 827026-45-9 is helpful to your research.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem