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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

Discovery of H-D-Pro-OH

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Using CRISPR-Cas9-mediated genome editing to generate C. difficile mutants defective in selenoproteins synthesis

Clostridium difficile is a significant concern as a nosocomial pathogen, and genetic tools are important when analyzing the physiology of such organisms so that the underlying physiology/pathogenesis of the organisms can be studied. Here, we used TargeTron to investigate the role of selenoproteins in C. difficile Stickland metabolism and found that a TargeTron insertion into selD, encoding the selenophosphate synthetase that is essential for the specific incorporation of selenium into selenoproteins, results in a significant growth defect and a global loss of selenium incorporation. However, because of potential polar effects of the TargeTron insertion, we developed a CRISPR-Cas9 mutagenesis system for C. difficile. This system rapidly and efficiently introduces site-specific mutations into the C. difficile genome (20-50% mutation frequency). The selD CRISPR deletion mutant had a growth defect in protein-rich medium and mimicked the phenotype of a generated TargeTron selD mutation. Our findings suggest that Stickland metabolism could be a target for future antibiotic therapies and that the CRISPR-Cas9 system can introduce rapid and efficient modifications into the C. difficile genome.

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

Awesome and Easy Science Experiments about H-D-Pro-OH

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A Pair of Rare Three-Dimensional Chiral Polyoxometalate-Based Metal-Organic Framework Enantiomers Featuring Superior Performance as the Anode of Lithium-Ion Battery

Two rare three-dimensional (3D) chiral polyoxometalate-based metal-organic framework (POMOF) materials, d- [PMo8VMo4VIO37(OH)3Zn4][BPP]2¡¤2[pyridine]¡¤H2O (d-1) and l-[PMo8VMo4VIO37(OH)3Zn4][BPP]2¡¤2[pyridine]¡¤H2O (l-1) (BPP = 1,3-bis(4-pyridyl)propane) were prepared with achiral ligand under solvothermal conditions. They are the first 3D chiral POM-based frameworks based on a Zn-?-Keggin unit and achiral ligands. The CD spectra and structural analyses indicate that the two polyoxometalate-based metal-organic frameworks are enantiomers. The alternate connection of Zn-?-Keggin cluster and BPP ligands generate helical infinite chains, while each single spiral chain is further interlinked to adjacent neighboring units to produce a 3D regular ordered chiral architecture with a qtz topology. Compound 1 (mixtures of d-1 and l-1) exhibited excellent stability in both acid and base aqueous solutions. When compound 1 was used as an anode electrode material of rechargeable Li-ion batteries (LIBs), outstanding reversible capacity of 1004 mA h g-1 was obtained after 100 cycles along with cycle stability and outstanding rate performance. Such a high reversible capacity has previously never been reported for the LIB anodes within the pristine POM-based crystals.

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

Properties and Exciting Facts About 4408-64-4

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 4408-64-4, name is 2,2′-(Methylazanediyl)diacetic acid, introducing its new discovery. Recommanded Product: 4408-64-4

Synthesis, characterization and antitumor activity of a series of diorganotin(IV) derivatives of bis(carboxymethyl)amines

A series of diorganotin(IV) derivatives of bis(carboxymethyl)amine and its N-methyl derivative have been prepared, characterized by NMR, Moessbauer and mass spectrometry and tested in vivo against P388 leukemia.

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

Discovery of 3105-95-1

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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

Extracurricular laboratory:new discovery of 2,2′-(Methylazanediyl)diacetic acid

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 4408-64-4, help many people in the next few years.Computed Properties of C5H9NO4

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Computed Properties of C5H9NO4, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 4408-64-4, Name is 2,2′-(Methylazanediyl)diacetic acid, molecular formula is C5H9NO4. In a Article, authors is Woerly, Eric M.£¬once mentioned of 4408-64-4

(1-Bromovinyl)-MIDA boronate: A readily accessible and highly versatile building block for small molecule synthesis Dedicated to Professor Paul Wender with deepest admiration on his receipt of the 2012 Tetrahedron Prize for Creativity in Organic Chemistry

Iterative cross-coupling represents a potentially general approach for the simple, efficient, and flexible construction of a wide range of functional small molecules. In this context, (1-bromovinyl)-N-methyliminodiacetic acid (MIDA) boronate is a very useful building block for small molecule synthesis. This compound can serve as a starting material for the preparation of a wide range of 1,1-disubstituted olefin-containing MIDA boronates. This compound can also be used for the iterative cross-coupling-based synthesis of various 1,1-disubstituted olefin-containing targets. Collectively, these results contribute to the expanding generality of the MIDA boronate platform.

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

Awesome and Easy Science Experiments about (1R,2R)-Cyclohexane-1,2-diamine

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 20439-47-8, name is (1R,2R)-Cyclohexane-1,2-diamine, introducing its new discovery. Formula: C6H14N2

Cooperative Al(salen)-pyridinium catalysts for the asymmetric synthesis of trans-configured beta-lactones by [2+2]-cyclocondensation of acylbromides and aldehydes: Investigation of pyridinium substituent effects

The trans-selective catalytic asymmetric formation of beta-lactones constitutes an attractive surrogate for anti-aldol additions. Recently, we have reported the first catalyst which is capable of forming trans-beta-lactones with high enantioselectivity from aliphatic (and aromatic) aldehyde substrates by cyclocondensation with acyl bromides. In that previous study the concepts of Lewis acid and organic aprotic ion pair catalysis were combined in a salen-type catalyst molecule. Since a pyridinium residue on the salen periphery is essential for high trans- and enantioselectivity, we were interested in the question of whether substituents on the pyridinium rings could be used to further improve the catalyst efficiency, as they might have a significant impact on the effective charges within the heterocycles. In the present study we have thus compared a small library of aluminum salen/bispyridinium catalysts mainly differing in the substituents on the pyridinium residues. As one result of these studies a new catalyst was identified which offers slightly superior stereoselectivity as compared to the previously reported best catalyst. NBO calculations have revealed that the higher stereoselectivity can arguably not be explained by the variation of the effective charge.

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

The important role of 1,4,7-Triazacyclononane

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Onchocerciasis in Yemen: Time to take action against a neglected tropical parasitic disease

Onchocerciasis is a neglected parasitic disease affecting the poorest underserved people in Yemen. A national control programme with goals to eliminate onchocerciasis has yet to be launched due to the current upheaval and social unrest in the country. The disease, locally termed as sowda, is unique in its clinicopathologic pattern, being of the localized, non-blinding, hyperreactive onchocercal skin disease. Although early reports identified endemic foci along seasonal watercourses, there is a need to redefine its epidemiologic patterns as well as health and socioeconomic impacts. Laboratory diagnosis of sowda among Yemeni patients is difficult due to the low load of microfilariae in skin snips and the presence of asymptomatic itching-free microfilaria carriers. Adoption of ivermectin use at three-month intervals as a control strategy has not been evaluated because the drug is mostly used in clinics and distributed to only a few affected communities. This paper addresses key aspects of onchocerciasis in Yemen and highlights the need for screening at-risk populations using highly sensitive techniques and mapping the distributions of the parasite in human and vector populations of blackflies. The new research should be integrated with the launch of a national onchocerciasis control programme to achieve onchocerciasis elimination.

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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

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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

Extracurricular laboratory:new discovery of 51207-66-0

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Substituted phenyl compounds with immunosuppressing activity and pharmaceutical compositions

The invention provides substituted phenyl compounds of general formula STR1wherein R 1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

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