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The heterogeneously catalyzed diastereoselective hydrogenation of furan-2-carboxylic acid derivatives modified with chiral auxiliaries is described. Chiral auxiliaries, catalysts, solvents, and additives were optimized for the reaction. Finally, the hydrogenation of furan-2-yl-[(S)-2- (hydroxydiphenylmethyl)-pyrrolidin-1-yl]-methanone resulted in a high diastereoselectivity. Removal of the auxiliary gave the tetrahydrofuran-2- carboxylic acid in 95% ee. Georg Thieme Verlag Stuttgart.

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N-Propargylamides having chiral centers at the alpha-carbon of the amide groups, 1-3, were polymerized with (nbd)Rh+[eta6-C6H5B-(C 6H5)3] to afford polymers with moderate molecular weights (Mn = 6000-32 000) in good yield. The 1H NMR spectra demonstrated that the polymers have stereoregular structures (cis = 100%). The polymers were proven to take a helical conformation with an excess of one- handed screw sense in CHCl3, which was supported by their intense CD effects and large optical rotations. It was confirmed that the helical structure was stabilized not only by the steric repulsion but also by the intramolecular hydrogen bonds between the pendant groups. CD spectroscopic study showed that the helical structure is more stable than that of the polymers without a branch at the alpha-position, which allowed the polymers to exist in the helical state in various solvents. The electronic absorption, CD effects, and optical rotations of the polymers closely correlated to the extent of the hydrogen bonding between the pendant amide groups.

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Clickable copycat! Readily available dipeptide d-Pra-epsilon-Lys is identified using a modified fluorescence protein assay as a highly efficient clickable pyrrolysine mimic. It is shown to incorporate into calmodulin in high yield to provide a handle for labeling with anazide-containing coumarin.

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This invention relates to compounds of formula (I), their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.

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A matched and mixed capping SAR study was conducted on the tetracyclic indole class of HCV NS5A inhibitors to examine the influence of modifications of this region on the overall HCV virologic resistance profiles.

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This application relates to substituted benzimidazoles of formula (I), compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to substituted benzimidazoles and to their use as bromodomain inhibitors. The present application also relates to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasm, including tumors and/or cancers.

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The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

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The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formula (I) or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

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The present invention provides compounds, compositions thereof, and methods of using the same.

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Tetrahydrofuran – Wikipedia,
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