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In the brains of patients with Alzheimer’s disease, the enzymatic activities of butyrylcholinesterase (BChE) and monoamine oxidase B (MAO-B) are increased. While BChE is a viable therapeutic target for alleviation of symptoms caused by cholinergic hypofunction, MAO-B is a potential therapeutic target for prevention of neurodegeneration in Alzheimer’s disease. Starting with piperidine-based selective human (h)BChE inhibitors and propargylamine-based MAO inhibitors, we have designed, synthesized and biochemically evaluated a series of N-propargylpiperidines. All of these compounds inhibited hBChE with good selectivity over the related enzyme, acetylcholinesterase, and crossed the blood-brain barrier in a parallel artificial membrane permeation assay. The crystal structure of one of the inhibitors (compound 3) in complex with hBChE revealed its binding mode. Three compounds (4, 5, 6) showed concomitant inhibition of MAO-B. Additionally, the most potent hBChE inhibitor 7 and dual BChE and MAO-B inhibitor 6 were non-cytotoxic and protected neuronal SH-SY5Y cells from toxic amyloid beta-peptide species.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H3301N – PubChem

 

Discovery of 2-Phenylpiperidine

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Several 5-HT(ID/1B) receptor agonists are now entering the marketplace as treatments for migraine. This paper describes the development of selective h5-HT(1D)receptor agonists as potential antimigraine agents which may produce fewer side effects. A series of 3-[3-(piperidin-1-yl)propyl]indoles has been synthesized which has led to the identification of 80 (L-772,405), a high- affinity h5-HT(1D) receptor full agonist having 170-fold selectivity for h5- HT(1D) receptors over h5-HT(1B) receptors. L-772,405 also shows very good selectivity over a range of other serotonin and nonserotonin receptors and has excellent bioavailability following subcutaneous administration in rats. It therefore constitutes a valuable tool to delineate the role of h5-HT(1D) receptors in migraine. Molecular modeling and physical properties have been utilized to postulate the binding conformation of these compounds in the receptor cavity.

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Piperidine – Wikipedia,
Piperidine | C5H9277N – PubChem

 

New explortion of tert-Butyl piperidin-4-ylcarbamate

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Reference of 73874-95-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.73874-95-0, Name is tert-Butyl piperidin-4-ylcarbamate, molecular formula is C10H20N2O2. In a Article,once mentioned of 73874-95-0

Ezetimibe (Zetia), a cholesterol-absorption inhibitor (CAI) approved by the FDA for the treatment of hypercholesterolemia, is believed to target the intestine protein Niemann-Pick C1-Like 1 (NPC1L1) or its pathway. A spiroimidazolidinone NPC1L1 inhibitor identified by virtual screening showed moderate binding activity but was not efficacious in an in vivo rodent model of cholesterol absorption. Synthesis of analogs established the structure-activity relationships for binding activity, and resulted in compounds with in vivo efficacy, including 24, which inhibited plasma cholesterol absorption by 67% in the mouse, thereby providing proof-of-concept that non-beta-lactams can be effective CAIs.

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Piperidine – Wikipedia,
Piperidine | C5H14215N – PubChem

 

Brief introduction of 137076-22-3

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Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H16425N – PubChem

 

More research is needed about 56346-57-7

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Related Products of 56346-57-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.56346-57-7, Name is (4-Fluorophenyl)(piperidin-4-yl)methanone, molecular formula is C12H14FNO. In a Article,once mentioned of 56346-57-7

A novel series of anti-malarials, based on a hydroxy-ethyl-amine scaffold, initially identified as peptidomimetic protease inhibitors is described. Combination of the hydroxy-ethyl-amine anti-malarial phramacophore with the known Mannich base pharmacophore of amodiaquine (57) resulted in promising in vivo active novel derivatives.

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Piperidine – Wikipedia,
Piperidine | C5H15519N – PubChem

 

More research is needed about 2-(2,6-Dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione

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The present invention relates to is suitable for industrial production of high-purity anchors ma duan preparation method, 3 – nitro phthalic anhydride with the glutamic acid reaction intermediates, in acetic anhydride under the conditions of the intermediate obtained in the reaction, under the conditions of the reaction in DMSO to obtain 3 – nitro – N – (2, 6 – dioxo – 3 – piperidinyl) phthalimide, palladium hydrocarbon obtained through anchors ma duan, this process has high yield, the operation is simple, environment friendly, and is suitable for mass production and the like, adopts low-toxicity solvent has been solved because the solvent residue caused by the problem of the unqualified products. (by machine translation)

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Piperidine – Wikipedia,
Piperidine | C5H23199N – PubChem

 

More research is needed about 2213-43-6

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2213-43-6, molcular formula is C5H12N2, introducing its new discovery. COA of Formula: C5H12N2

The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I) wherein R and R1-R4 have the meanings given in the specification.

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Piperidine – Wikipedia,
Piperidine | C5H748N – PubChem

 

Awesome Chemistry Experiments For 145508-94-7

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Chemistry is traditionally divided into organic and inorganic chemistry. COA of Formula: C11H20INO2. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 145508-94-7

Pleiotropic intervention may be a requirement for effective limitation of the progression of multifactorial diseases such as Alzheimer’s Disease. One approach to such intervention is to design a single chemical entity capable of acting on two or more targets of interest, which are accordingly known as Multi-Target Directed Ligands (MTDLs). We recently described donecopride, the first MTDL able to simultaneously inhibit acetylcholinesterase and act as an agonist of the 5-HT4 receptor, which displays promising activities in vivo. Pharmacomodulation of donecopride allowed us to develop a novel series of indole derivatives possessing interesting in vitro activities toward AChE and the sigma1 receptor. The crystal structures of complexes of the most promising compounds with Torpedo californica AChE were solved in order to further understand their mode of inhibition.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H23610N – PubChem

 

Archives for Chemistry Experiments of 39546-32-2

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The invention provides a liquid crystal aligning agent, liquid crystal alignment film, the liquid crystal display element, phase difference film and method of manufacturing the same, polymer and compound. The present invention provides a voltage retention can be obtained various properties such as good liquid crystal display element of the liquid crystal aligning agent. In the liquid crystal aligning agent of the present invention having the following formula (1) a structure represented by the polymer (P) as a polymer component. (R1 Is a hydrogen atom or carbon number 1 – 30 of 1 monovalent hydrocarbon radical, X1 And X2 Is independently 2 monovalent organic radical; 2 a with “*” are different from each other of said bonded bonding group). (by machine translation)

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Piperidine – Wikipedia,
Piperidine | C5H3468N – PubChem

 

New explortion of N-Carbethoxy-4-piperidone

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 29976-53-2, molcular formula is C8H13NO3, introducing its new discovery. Recommanded Product: 29976-53-2

In one aspect, the invention relates to novel bicyclic oxazole and thiazole compounds which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions; and methods for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention

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Piperidine – Wikipedia,
Piperidine | C5H10076N – PubChem