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SERINE PROTEASES, THEIR ACTIVITY AND THEIR SYNTHETIC INHIBITORS

The present invention relates to new compounds of the general formula: Z-Xaa-Y’, in which Xaa is an amino acid, Z is a protecting group and Y’ is one of various types of ring structures. The new compounds have a modulating activity on serine proteases. The invention further relates to the use of the compounds in therapy and diagnosis and to a method of purifying the serine protease DPPIV.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Synthetic Route of 3105-95-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.3105-95-1, Name is H-HoPro-OH, molecular formula is C6H11NO2. In a Patent£¬once mentioned of 3105-95-1

BICYCLIC UNSATURATED TERTIARY AMINE COMPOUND

The present invention provides a bicyclic unsaturated tertiary amine compound capable of inhibiting the production of inflammatory cytokines.A compound of the following formula (1): (wherein, A represents pyrrole or pyrazole, R1 represents an aryl group or a heteroaryl group which may be substituted, R2 represents a heteroaryl group which may be substituted, and R3 represents an indolizine group), or a pharmacologically acceptable salt thereof, a pharmacologically acceptable ester thereof or other pharmacologically acceptable derivative thereof.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Stereoselective synthesis of (+)-and (-)-lentiginosine

Simple routes to (1R,2R,8aR)- and (1S,2S,8aS)-lentiginosine have been described, based on Sharpless asymmetric dihydroxylation, starting from (R)- and (S)-pipecolinic acids.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 3105-95-1, help many people in the next few years.Formula: C6H11NO2

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Process of making optically pure L-pipecolic acid and process of making anesthetics and intermediates therefrom

The present invention describes a novel process of preparation of optically pure L-Pipecolic acid and an improved process for the conversion of L-pipecolic acid to L-N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide, its hydrochloride salt and hydrochloride monohydrate.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Restricted conformation analogues of an anthelmintic cyclodepsipeptide

Six analogues of the anthelmintic cyclodepsipeptide PF1022A were prepared, each containing a small ring fused to the macrocycle to restrict the number of conformations the larger ring can adopt. It was anticipated that such conformational changes could lead to enhanced biological activity and selectivity. The analogues form two series of three members each. In one series, a carbon-based molecular bridge joins the methyl of a leucine residue with the methyl of its closest lactic acid residue to form five-, six-, and seven-membered lactam rings. In the second series, a leucine residue is replaced with five-, six-, and seven-membered nitrogen heterocycles. Decreasing the size of the small ring in the lactam series increasingly distorts the macrocycle and consistently decreases activity relative to PF1022A. In the leucine series, a similar trend is observed. Molecular modeling of PF1022A along with the analogues described herein suggests that the ability to exist in a highly symmetrical conformational state is a necessary condition for biological activity.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

Can You Really Do Chemisty Experiments About H-HoPro-OH

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 3105-95-1, help many people in the next few years.Product Details of 3105-95-1

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Product Details of 3105-95-1, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 3105-95-1, Name is H-HoPro-OH, molecular formula is C6H11NO2. In a Patent, authors is £¬once mentioned of 3105-95-1

Compounds possessing neuronal activity

The present invention relates to compounds, methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compounds and the compositions and methods that utilize them can be used, either alone or in conjunction with a neurotrophic factor, such as nerve growth factor, to promote repair of neuronal damage caused by disease or physical trauma.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Computed Properties of C6H11NO2, you can also check out more blogs about3105-95-1

Chemistry is traditionally divided into organic and inorganic chemistry. Computed Properties of C6H11NO2. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 3105-95-1

PROCESS FOR PRODUCING PIPECOLAMIDE DERIVATIVE

A method of manufacturing a pipecolamide derivative, characterized in that pipecolic acid or an acid salt thereof is reacted with an amine in an inert solvent in the presence of a condensing agent such as dicyclohexylcarbodiimide, 1-ethyl- 2-(2-dimethylaminopropyl) carbodiimide, methanesulfonyl chloride or phosphoryl chloride. Pipecolamide derivatives, particularly in optically active forms thereof can be efficiently and economically manufactured without harmful gas by-products.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Synthesis of new perhydropyrrolo[1,2-A]pyrazine derivatives and their evaluation in animal models of epilepsy

A series of novel stereochemically pure derivatives of the investigative broad-spectrum anticonvulsant ADD408003 was designed and synthesized. Five-center four-component (U-5C-4CR) and four-center three-component (U-4C-3CR) variants of Ugi reaction were used in the key step of the synthetic pathways. The compounds obtained were evaluated for the anticonvulsant activitiy in the maximal electroshock seizure (MES), subcutaneous Metrazole (scMET) and minimal clonic seizure (6 Hz) animal models of epilepsy. The efficacies of most derivatives in the 6 Hz model of pharmacoresistant partial seizures were markedly higher than in the ‘classical’ MES and scMET models. The most active compounds, (4R,8aR)-3a, and (4S,8aS)-6 displayed median effective doses (ED50) of 47.90 and 126.19 mg/kg, respectively, for the 6 Hz test.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Tandem radical decarboxylation-oxidation of amino acids: A mild and efficient method for the generation of N-acyliminium ions and their nucleophilic trapping

A convenient methodology for the synthesis of 2-substituted pyrrolidines from alpha-amino acids is described. A number of cyclic and acyclic alpha-amino acid derivatives have been prepared in order to test the scope and diastereoselectivity of this method. These substrates were treated with iodosylbenzene or (diacetoxyiodo)benzene (DIB) and iodine in order to generate the corresponding carboxyl radical, which evolves by loss of carbon dioxide to produce a carbon radical which in turn undergoes oxidation to an N-acyliminium ion. This postulated intermediate could be trapped inter- or intramolecularly by oxygen, nitrogen and carbon nucleophiles. In the case of carbon nucleophiles, a Lewis acid is required for the concomitant carbon-carbon bond formation. High yields and modest diastereoselectivities were obtained. The present methodology was applied to the synthesis of omega-amino aldehydes or hemiaminals 8-14, 2-aminopyrrolidine derivative 15, aminolactone derivative 16, and azasugar analogues 17 and 18. When carbon nucleophiles were used, alkaloid precursors such as 2-allyl- or 2-alkylpyrrolidines 19-23 and 25 were obtained.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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NOVEL DUAL NK2/NK3-ANTAGONISTS, PHARMACEUTICALCOMPOSITIONS COMPRISING THEM AND PROCESSES FOR THEIR PREPARATIONS

The present invention relates to novel dual NK2/NK3-antagonists of formula (I) wherein the meaning of X and R1 to R5 is defined in the claims and in the description and also to pharmaceutical compositions comprising these compounds. Furthermore, the invention relates to processes for the preparation of the novel dual NK2/NK3-antagonists and to their uses.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI