- Effect of enzymatic sulfation on biochemical and pharmacological properties of catecholamines and tyrosine-containing peptides
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Substrate specificity of a novel sulfotransferase produced by Eubacterium A-44 isolated from human feces has been studied. Phenolic drugs, catecholamines, were good acceptors of this bacterial enzyme. With regard to dopamine, sulfation mostly occurred at
- Konishi-Imamura,Kim,Kobashi
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Read Online
- Tri- and tetravalent photoactivable cross-linking agents
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A modular synthesis of photoactivable cross-linking agents is described, using an aromatic core, di- or triethyleneglycol spacers and photoaffinity labeling synthons that feature either perfluorophenyl azide or aryl(trifluoromethyl)diazirine motifs. Symmetrical and nonsymmetrical trivalent structures were obtained from phloroglucinol and dopamine, respectively. Symmetrical tetravalent structures resulted from the coupling of two dopamine derivatives with oxalyl chloride. Georg Thieme Verlag Stuttgart New York.
- Welle, Alexandre,Billard, Francois,Marchand-Brynaert, Jacqueline
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supporting information; experimental part
p. 2249 - 2254
(2012/10/08)
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- Synthesis and biological studies of glycosyl dopamine derivatives as potential antiparkinsonian agents
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A new approach to deliver dopamine into the central nervous system, based on the use of D-glucose as transportable agent, has been studied. Glycosyl dopamine derivatives bearing the sugar moiety linked to either the amino group or the catechol ring of dopamine through amide, ester or glycosidic bonds were synthesised as potential antiparkinsonian agents. Studies on the binding to dopamine D2 receptor, in vitro stability, and locomotive effect in mice of the synthetic glycoconjugates are reported. Copyright (C) 2000 Elsevier Science Ltd.
- Fernandez, Caridad,Nieto, Ofelia,Rivas, Emilia,Montenegro, Gisela,Fontenla, Jose A.,Fernandez-Mayoralas, Alfonso
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p. 353 - 365
(2007/10/03)
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- Preparation for endermism containing dopamine derivatives
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(A) a diacylated dopamine derivative represented by the formula (I): STR1 wherein R1 represents an alkyl group having 3 to 7 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms, substituted or unsubstituted phenyl group or a substituted
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- O2-Cu2+-ASCORBIC ACID: A NOVEL OXIDATION SYSTEM FOR THE HIGHLY SELECTIVE O-DEALKYLATION OF 2-ALKOXYPHENOLS
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The novel oxidation system "O2-Cu2+-ascorbic acid" is a selective reagent for the oxidative O-dealkylation of 2-alkoxyphenols and affords catechols in good yield.KEYWORDS - O-dealkylation; ascorbic acid; copper ion; oxidation; 2-alkoxyphenol; vanillin; dopamine; guaiacol; catechol
- Aihara, Kazuhiro,Higuchi, Tsunehiko,Hirobe, Masaaki
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p. 837 - 840
(2007/10/02)
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- Method for improving the absorption and effectiveness of a catecholamine compound
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A catecholamine compound is converted to a new mono O-phosphate ester derivative thereof which exhibit improved absorption and effectiveness.
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- Synthesis and chemical properties of ibopamine and of related esters of N-substituted dopamines - Synthesis of ibopamine metabolites
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The therapeutic usefulness of intravenously infused dopamine in congestive heart failure and in shock prompted us to synthesize a wide series of 3,4-O-diesters of dopamine and N-substituted derivatives to obtain an orally active dopamine-like prodrug having adequate absorption and duration of action. The pharmacological results and in particular, the hemodynamic studies in the dog led to the selection of ibopamine, i.e. the 3,4-diisobutyryl ester of N-methyldopamine and to its development as a useful drug for the chronic treatment of congestive heart failure. The choice of ibopamine from among several analogs was also influenced by other favourable properties such as good chemical stability in pharmaceutical formulations and in the biopharmaceutical phases of the absorption, and fast enzymatic activation of the prodrug by plasma and peripheral tissue esterases; the latter property appeared desirable to avoid any accumulation in the central nervous system and consequent undesired side effects. The isomeric mixture of 3-O- and 4-O- isobutyrates of N-methyldopamine as well as the main conjugated metabolites, i.e. the 3-O- and 4-O-sulphate and 4-O-β-glucuronide of N-methyldopamine were synthesized as analytical references in metabolic studies and for the investigation of their pharmacokinetic and pharmacological properties. Dopamine O-sulphates were also prepared using the methods developed for the corresponding N-methyl derivatives.
- Casagrande,Santangelo,Saini,Doggi,Gerli,Cerri
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p. 291 - 303
(2007/10/02)
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- 3,4- AND 3,5-Dialkoxybenzylamines
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Novel benzyl- and phenylethylamines useful as anti-viral agents are claimed as well as a process and a pharmaceutical composition for combating viral infections.
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