- Synthesis of amino acid derivatives of hydrazones and oximes of spirodihydropyranochromen-2-ones
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Sulfur-and nitrogen-containing derivatives of spirodihydropyranochromen-2- ones at the exocyclic oxygen atom have been synthesized. Modification of the oximes and hydrazones of the spiro-substituted pyranocoumarins with N-substituted amino acids were carried out using activated ester and symmetrical anhydride methods.
- Veselovska,Garazd,Ogorodniychuk,Garazd,Khilya
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experimental part
p. 153 - 162
(2009/04/03)
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- Novel compositions for the delivery of negatively charged molecules
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This invention features permeability enhancer molecules, and methods, to increase membrane permeability of various molecules, such as nucleic acids, polynucleotides, oligonucleotides, enzymatic nucleic acid molecules, antisense nucleic acid molecules, 2-5A antisense chimeras, triplex forming oligonucleotides, decoy RNAs, dsRNAs, siRNAs, aptamers, or antisense nucleic acids containing nucleic acid cleaving chemical groups, peptides, polypeptides, proteins, carbohydrates, steroids, metals and small molecules, thereby facilitating cellular uptake of such molecules.
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- Compositions for the delivery of negatively charged molecules
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This invention features permeability enhancer molecules, and methods, to increase membrane permeability of negatively charged polymers thereby facilitating cellular uptake of such polymers.
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- An Easy Preparation of Hapten Active Esters via Solid Supported EDAC
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Bioconjugates are preferably prepared by reacting an active ester of the hapten of interest to the protein.Preparation of active esters with solid supported EDAC and N-hydroxysuccinimide or pentafluorophenol affords active esters in excellent yield and pu
- Adamczyk, Maciej,Fishpaugh, Jeffrey R.,Mattingly, Phillip G.
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p. 8345 - 8346
(2007/10/02)
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- Structure-Activity Relationships of Dopaminergic 5-Hydroxy-2-aminotetralin Derivatives with Functionalized N-Alkyl Substituents
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5-Hydroxy-2-aminotetralin derivatives in which one N-alkyl substituent carries a functional group have been prepared and their dopaminergic activities compared with those of 5-hydroxy-2-(di-n-propylamino)tetralin (5-OH-DPAT) and known ergolines.Several members of the series demonstrated high affinities in dopamine (DA) receptor binding and DA agonist properties in the rotational behavior model in the range of known potent ergolines.The results suggests that the accessory binding site for the larger N-alkyl substituent of the 5-hydroxy-2-aminotetralins can accommodate various neutral and bulky functionalities and is probably identical with the site(s) to which the 8-substituents of the ergolines bind.
- Seiler, Max P.,Stoll, Andre P.,Closse, Annemarie,Frick, Willy,Jaton, Annelise,Vigouret, Jean-Marie
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p. 912 - 917
(2007/10/02)
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