Scoping the Enantioselective Desymmetrization of a Poorly Water-Soluble Diester by Recombinant Pig Liver Esterase
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چکیده
منابع مشابه
Nanosized Technological Approaches for the Delivery of Poorly Water Soluble Drugs
A major hurdle in pharmaceutical formulation is water insolubility of most of drugs affecting their stability and bioavailability. If the drug is also insoluble in organic medium, it is difficult to deliver it in a sufficiently bioavailable form and hence it is a great challenge to formulation researchers to overcome such difficulty. Although some approaches are available for enhancing th...
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Solid dispersions have been employed to enhance the dissolution rates of poorly water-soluble drugs. Many approaches have been investigated for the preparation of solid dispersions. This paper reports the various solubility enhancement strategies in solid dispersion. The approaches described are fusion (melting), solvent evaporation, lyophilization (freeze drying), melt agglomeration process, e...
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The solubilizing ability of two aromatic hydrotropes, N,N-diethylnicotinamide (DENA) and N,N-dimethylbenzamide (DMBA), was investigated using a set of 13 poorly soluble, structurally diverse drugs. The number of aromatic rings in the solute molecule has a very strong effect on the solubility enhancement produced by either hydrotrope. However, although solubility enhancements in the order of 100...
متن کاملSubstrate-Enzyme Interaction in Pig Liver Esterase
Force field and first principles molecular dynamics simulations on complexes of pig liver esterase (pig liver isoenzymes and a mutant) and selected substrates (1-phenyl-1-ethyl acetate, 1phenyl-2-butylacetate, proline-β-naphthylamide and methyl butyrate) are presented. By restrained force field simulations the access of the substrate to the hidden active site was probed. For a few substrates sp...
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An amino-indanol derived chiral guanidine was developed as an efficient Brønsted base catalyst for the desymmetrization of meso-aziridines with both thiols and carbamodithioic acids as nucleophiles, which provided 1,2-difunctionalized ring-opened products in high yields and enantioselectivities.
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ژورنال
عنوان ژورنال: Organic Process Research & Development
سال: 2018
ISSN: 1083-6160,1520-586X
DOI: 10.1021/acs.oprd.8b00277