- COMPOSITIONS AND METHODS FOR SINGLE-STEP MULTIPURPOSE SURFACE FUNCTIONALIZATION
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Compositions and methods for functionalizing a variety of surfaces are provided herein. The compositions include compounds of formula (I), which react with azido compounds (R-N3) to form cycloadducts that can spontaneously polymerize on a surfa
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Page/Page column 40; 41
(2021/07/02)
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- Targeted double-stimulation responsiveness multifunction cerium dioxide nano-medicine carrying system capable of degrading polydopamine packs
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The invention relates to a targeted double-stimulation responsiveness multifunction cerium dioxide nano-medicine carrying system capable of degrading polydopamine packs. According to the system, cerium dioxide with cytotoxicity serves as a medicine carryi
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Paragraph 0038; 0039; 0040
(2018/03/25)
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- Water-soluble L-DOPA esters
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The present invention relates to novel compounds of the formula I, methods for their preparation and their use for treatment of diseases. The invention discloses the synthesis of levodopa (L-DOPA) esters by coupling polyhydroxy compounds or their derivatives to the L-DOPA carboxyl group. The synthesis allows to produce L-DOPA derivatives which are highly soluble in water as well as aqueous and biocompatible liquids and have an improved hydrolytic stability in water or aqueous and biocompatible media for an application over several days. The invention helps producing L-DOPA substances for applications in the fields of medicine, biology and medical engineering as well as in the pharmaceutical industry.
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Paragraph 0089
(2018/05/24)
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- The design and evaluation of an l-dopa–lazabemide prodrug for the treatment of Parkinson’s disease
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L-Dopa, the metabolic precursor of dopamine, is the treatment of choice for the symptomatic relief of the advanced stages of Parkinson’s disease. The oral bioavailability of L-dopa, however, is only about 10% to 30%, and less than 1% of the oral dose is estimated to reach the brain unchanged. L-Dopa’s physicochemical properties are responsible for its poor bioavailability, short half-life and the wide range of inter- and intrapatient variations of plasma levels. An L-dopa–lazabemide prodrug is proposed to overcome the problems associated with L-dopa absorption. Lazabemide is a monoamine oxidase (MAO)-B inhibitor, a class of compounds that slows the depletion of dopamine stores in Parkinson’s disease and elevates dopamine levels produced by exogenously administered L-dopa. L-Dopa was linked at the carboxylate with the primary aminyl functional group of lazabemide via an amide, a strategy which is anticipated to protect L-dopa against peripheral decarboxylation and possibly also enhance the membrane permeability of the prodrug. Selected physicochemical and biochemical properties of the prodrug were determined and included lipophilicity (logD), solubility, passive diffusion permeability, pKa, chemical and metabolic stability as well as cytotoxicity. Although oral and i.p. treatment of mice with the prodrug did not result in enhanced striatal dopamine levels, 3,4-dihydroxyphenylacetic acid (DOPAC) levels were significantly depressed compared to saline, L-dopa and carbidopa/L-dopa treatment. Based on the results, further preclinical evaluation of the L-dopa–lazabemide prodrug should be undertaken with the aim of discovering prodrugs that may be advanced to the clinical stages of development.
- Hoon, Monique,Petzer, Jacobus P,Viljoen, Francois,Petzer, Anél
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- Synthesis of peptides containing DOPA (3,4-dihydroxyphenylalanine)
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Proteins from coral reefs structures, eggshells, and marine mollusk adhesives all contain the amino acid 3,4-dihydroxyphenylalanine (DOPA). The insoluble nature of these materials has hampered characterization and turned our efforts toward work with small peptide mimics. In this paper, we present the syntheses of various DOPA derivatives: Boc-DOPA, Fmoc-DOPA, DOPA(TBDMS)2, DOPA(TBDPS)2, Boc-DOPA(TBDPS)2, Fmoc-DOPA(TBDMS)2, and Fmoc-DOPA(TBDPS)2 (where Boc=tert-butyloxycarbonyl, Fmoc=9-fluorenylmethyloxycarbonyl, TBDMS=tert-butyldimethylsilyl, and TBDPS=tert-butyldiphenylsilyl). These DOPA compounds were used to prepare peptides of various sequences. The synthetic procedure described provides an efficient route to DOPA-containing peptides in which sidechain deprotection and cleavage from resin can be accomplished in one step.
- Sever, Mary J,Wilker, Jonathan J
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p. 6139 - 6146
(2007/10/03)
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- A New Convenient Route for the Synthesis of DOPA Peptides
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The tert-butyldimethylsilyl group as the catechol protective group of DOPA (compound 1a), Boc-DOPA (compound 1b) and DOPA esters (compounds 2a-c) is introduced.The compounds 2a-c and 1b are used as the starting substrates for the synthesis of the protecte
- Nakonieczna, Lucja,Przychodzen, Witold,Chimiak, Andrzej
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p. 1055 - 1058
(2007/10/02)
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