23/9/2021 News Some scientific research about 4138-26-5

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A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H3321N – PubChem

 

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This invention relates to certain pyrimidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

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Piperidine – Wikipedia,
Piperidine | C5H3252N – PubChem

 

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Chemistry is traditionally divided into organic and inorganic chemistry. Computed Properties of C6H12N2O. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 4138-26-5

A series of C-5 methyl substituted 4-arylthio- and 4-aryloxy-3-iodopyridin- 2(1H)-ones has been synthesized as new pyridinone analogues for their evaluation as anti-HIV inhibitors. The optimization at the 5-position was developed through an efficient use of the key intermediates 5-ethoxycarbonyl- and 5-cyano-pyridin-2(1H)-ones (14 and 15). Biological studies revealed that several compounds show potent HIV-1 reverse transcriptase inhibitory properties, for example, compounds 93 and 99 are active at 0.6-50 nM against wild type HIV-1 and a panel of major simple/double HIV mutant strains.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H3319N – PubChem

 

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A method has been developed for the synthesis of 4-amino-substituted 7-benzyl-2-morpholin-4-yl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidines by condensation of ethyl 1-benzyl-3-oxopiperidine-4-carboxylate with morpholine-4-carboxamidine and subsequent reaction of the 7-benzyl-2-morpholin- 4-yl-5,6,7,8-tetrahydro-3H-pyrido[3,4-d]pyrimidin-4-one with trifluoromethanesulfonic anhydride and secondary amines.

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Piperidine – Wikipedia,
Piperidine | C5H3330N – PubChem

 

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Electric Literature of 4138-26-5, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 4138-26-5, name is Piperidine-3-carboxamide. In an article,Which mentioned a new discovery about 4138-26-5

The solubilities of five poorly water-soluble drugs, diazepam, griseofulvin, progesterone, 17beta-estradiol, and testosterone, were studied in the presence of nicotinamide. All solubilities were found to increase in a nonlinear fashion as a function of nicotinamide concentration. The K(1:1) and K(1:2) stability constants were as follows: for diazepam, K(1:1) = 5.23 M-1 and K(1:2) = 8.6 M-2; for griseofulvin, K(1:1) = 5.54 M-1 and K(1:2) = 8.82 M-2; for progesterone, K(1:1) = 5.48 M-1 and K(1:2) = 42.47 M-2; for 17beta-estradiol, K(1:1) = 5.38 M-1 and K(1:2) = 36.9 M-2; and for testosterone, K(1:1) = 5.07 M-1 and K(1:2) = 27.47 M-2. Two aliphatic analogues of nicotinamide (nipecotamide and N,N-dimethylacetamide) were studied as ligands with diazepam and griseofulvin and were found to increase the solubilities of both drugs in a linear fashion. The aromatic analogue, N,N-diethylnicotinamide, showed a nonlinear solubilization relationship similar to that seen with nicotinamide. In addition, three other aromatic analogues (isonicotinamide, 1-methylnicotinamide iodide, and N-methylnicotinamide) were studied. These ligands were not soluble enough in water to be studied over the wide range of concentrations used for nicotinamide and N,N-diethylnicotinamide; however, in the concentration range studied, these ligands solubilized diazepam and griseofulvin to a degree similar to that observed with comparable concentrations of nicotinamide. These results suggest that the aromaticity (Pi-system) of the pyridine ring is an important factor in complexation because the aromatic amide ligands were found to enhance the aqueous solubilities of the test drugs to a greater extent than the aliphatic amide ligands. To determine if self-association of nicotinamide in water is required for its solubilization effects, the behavior of concentrated solutions of nicotinamide was studied. Solutions of nicotinamide in water up to 400 mg/mL were found to follow Beer’s Law, but there was a slight initial decrease in the surface tension followed by a plateau with increasing nicotinamide concentration. Conductivity was found to increase, and the NMR spectra showed an upfield chemical shift with increasing nicotinamide concentration. The n-octanol-water partition coefficient of nicotinamide was found to increase in a nonlinear fashion with increasing concentration. These results suggest that at high concentrations, nicotinamide undergoes slight self-association in water, but the degree of formation of higher order species was not sufficient to account for the degree of enhancement observed in the solubilities of the test compounds. Self-association may contribute to solubilization by affecting the hydrophobicity of the medium, but our data suggest that the aromaticity of the pyridine ring, which may promote the stacking of molecules through its planarity, appears to be the most significant contributor to the overall solubilization process. The solubilization appears to be due to formation of both 1:1 and 1:2 complexes between the drugs and nicotinamide.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H3257N – PubChem

 

The important role of Piperidine-3-carboxamide

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Pyrimido[5,4-d]pyrimidines of the general formula [Figure] which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are: 4-[(3-Chloro-4-fluorophenyl)amino]-6-[1-methyl-4-piperidinylamino]pyrimido[5,4-d]pyrimidine, and 4-[(3-Chloro-4-fluorophenyl)amino]-6-[trans-4-dimethyl-aminocycohexylamino]pyrimido[5,4-d]pyrimidine.

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Piperidine – Wikipedia,
Piperidine | C5H3287N – PubChem

 

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Application of 4138-26-5, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.4138-26-5, Name is Piperidine-3-carboxamide, molecular formula is C6H12N2O. In a article,once mentioned of 4138-26-5

The standard (p = 0.1 MPa) molar enthalpies of formation, at T = 298.15 K, in the gaseous phase, of three piperidinecarboxamide derivatives, namely 1-, 3- and 4-piperidinecarboxamide, were determined from their enthalpies of combustion and sublimation, obtained by static bomb calorimetry in oxygen and by Calvet microcalorimenty, respectively. The final results are analysed and discussed in terms of molecular structure.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H3256N – PubChem

 

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A series of non-imidazole histamine H3 receptor antagonists based on the (3-phenoxypropyl)amine motif, which is a common pharmacophore for H3 antagonists, has been identified. A preliminary SAR study around the amine moiety has identified 8a as a potent H3 antagonist possessing a good pharmacokinetic profile in the rat.

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Piperidine – Wikipedia,
Piperidine | C5H3318N – PubChem

 

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A series of oxindole CDK2 inhibitors was synthesized. These novel analogues have a saturated monosubstituted cyclic moiety at their C-4 position that mimics the ribofuranoside of ATP. This substitution afforded agents with increased potency relative to the parent indolinone and nanomolar range IC50 against the CDK2 enzyme and two cancer cell lines.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H3316N – PubChem

 

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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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Piperidine – Wikipedia,
Piperidine | C5H3301N – PubChem