Zobrazeno 1 - 10 of 13 pro vyhledávání: '"Michel Claesen"'
1
Ester prodrugs of ampicillin tailored for intracellular accumulation
Autor: Etienne Sonveaux, Isabelle Paternotte, M. Vermander, Pierre Dumont, Michel Claesen, K Li, B. Scorneaux, M. Beaujean, P. Osinski, HJ Fan, Paul M. Tulkens
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:3107-3112
Seven new ester prodrugs of ampicillin with hydrolysis half-lives ranging from 65 to 308 min were synthesized. The cellular accumulation of two of them (in J774 mouse macrophages) and their activities against intracellular Staphylococcus aureus were
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::522a58defc4b6b3f6ef34862d2529d61
https://doi.org/10.1016/s0960-894x(97)10146-9
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2
Syntheses and hydrolysis of basic and dibasic ampicillin esters tailored for intracellular accumulation
Autor: Etienne Sonveaux, Michel Claesen, Pascal Scrève, Isabelle Paternotte, Hua Juan Fan, Paul M. Tulkens
Publikováno v: Bioorganicmedicinal chemistry. 9(2)
Readily hydrolysable basic and dibasic esters of ampicillin were synthesised by alkylation of the carboxylate function of ampicillin to obtain prodrugs that may accumulate in cells and allow for an intracellular delivery of ampicillian (Fan et al., B
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e5c4e13bb8936636ecfbbed81c81c55
https://pubmed.ncbi.nlm.nih.gov/11249141
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3
A lymphotropic prodrug of L-dopa: synthesis, pharmacological properties and pharmacokinetic behavior of 1,3-dihexadecanoyl-2-[(S)-2-amino-3-(3,4-dihydroxyphenyl)propanoyl]propane-1,2,3-triol
Autor: Jacques H. Poupaert, Pierre Dumont, Michel Claesen, Aaron Garzon-Aburbeh
Publikováno v: Journal of Medicinal Chemistry. 29:687-691
A glyceride derivative of L-Dopa, 1,3-dihexadecanoyl-2-[(S)-2-amino-3-(3,4-dihydroxyphenyl)propan oyl] propane-1,2,3-triol (1), was synthesized and tested as an orally administrable prodrug endowed with lymphotropic properties. In the oxotremorine an
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca99ca2744de722b2d82687905540224
https://doi.org/10.1021/jm00155a018
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4
Absolute configuration of the major metabolite of 5,5-diphenylhydantoin,5-(4'-hydroxyphenyl)-5-phenylhydantoin
Autor: Michel Claesen, Pierre Dumont, Jacques H. Poupaert, Robert Cavalier
Publikováno v: Journal of Medicinal Chemistry. 18:1268-1271
Chemical conversions, optical comparisons, and chiroptical measurements (CD) were employed to determine the absolute configuration of the enantiomers of 5-(4'-hydroxyphenyl)-5-phenylhydantoin (HPPH) (1b and 1c). Studies on a key intermediate, (-)-2-c
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ea1dbaa92e7f33f68b37965062cdd2c
https://doi.org/10.1021/jm00246a024
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5
Stereochemical aspects of the metabolism of 5-(4'-fluorophenyl)-5-phenylhydantoin in the rat
Autor: Michel Claesen, Pierre Dumont, Jacques H. Poupaert, Pierre De Laey, Jacques Adline
Publikováno v: Journal of Medicinal Chemistry. 22:1140-1142
Racemic 5-(4'-fluorophenyl)-5-phenylhydantoin was synthesized to examine its metabolism in rat. This compound differs from the antiepileptic agent 5,5-diphenylhydantoin in that the normal site of hydroxylation in 5,5-diphenylhydantoin is blocked on o
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ed14388390618f5afefe59603c1d035
https://doi.org/10.1021/jm00195a029
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6
ChemInform Abstract: A Lymphotropic Prodrug of L-Dopa: Synthesis, Pharmacological Properties and Pharmacokinetic Behavior of 1,3-Dihexadecanoyl-2-[(S)-2-amino-3- (3,4-dihydroxyphenyl)propanoyl]propane-1,2,3-triol
Autor: Pierre Dumont, Jacques H. Poupaert, Michel Claesen, Aaron Garzon-Aburbeh
Publikováno v: Chemischer Informationsdienst. 17
A glyceride derivative of L-Dopa, 1,3-dihexadecanoyl-2-[(S)-2-amino-3-(3,4-dihydroxyphenyl)propan oyl] propane-1,2,3-triol (1), was synthesized and tested as an orally administrable prodrug endowed with lymphotropic properties. In the oxotremorine an
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6e95ff830edf2c13cc80aa19aa3751bb
https://doi.org/10.1002/chin.198638338
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8
ChemInform Abstract: ABSOLUTE CONFIGURATION OF THE MAJOR METABOLITE OF 5,5-DIPHENYLHYDANTOIN,5-(4′-HYDROXYPHENYL)-5-PHENYLHYDANTOIN
Autor: Robert Cavalier, Pierre Dumont, Michel Claesen, Jacques H. Poupaert
Publikováno v: Chemischer Informationsdienst. 7
Chemical conversions, optical comparisons, and chiroptical measurements (CD) were employed to determine the absolute configuration of the enantiomers of 5-(4'-hydroxyphenyl)-5-phenylhydantoin (HPPH) (1b and 1c). Studies on a key intermediate, (-)-2-c
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::14750ea8b2fc1a50a9c5c81911fe48a7
https://doi.org/10.1002/chin.197614185
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9
ChemInform Abstract: 1,3-DIPALMITOYLGLYCEROL ESTER OF CHLORAMBUCIL AS A LYMPHOTROPIC, ORALLY ADMINISTRABLE ANTINEOPLASTIC AGENT
Autor: Jacques Poupaert, Patrick Dumont, Aaron Garzon-Aburbeh, Michel Claesen, Ghanem Atassi
Publikováno v: Chemischer Informationsdienst. 14
A glyceride derivative of chlorambucil (2), 1,3-dipalmitoyl-2-[4-[bis (2-chloroethyl)amino]benzenebutanoyl]glycerol (1), was synthesized and tested as an orally administrable antineoplastic drug endowed with lymphotropic properties. A significantly h
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::996a1a30041e6f057b583a1af1667507
https://doi.org/10.1002/chin.198350127
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