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Titolo:
The synthesis of the glucuronide metabolite of UK-157,147 using immobilised uridine 5 '-diphosphoglucuronyl transferase and traditional organic chemistry techniques (imidate method)
Autore:
Webster, R; Beaumont, K; Ritzau, M; Stachulski, AV;
Indirizzi:
Pfizer Ltd, Cent Res, Dept Drug Metab, Sandwich CT13 9NJ, Kent, England Pfizer Ltd Sandwich Kent England CT13 9NJ andwich CT13 9NJ, Kent, England Pfizer Ltd, Cent Res, Dept Phys Sci, Sandwich CT13 9NJ, Kent, England Pfizer Ltd Sandwich Kent England CT13 9NJ andwich CT13 9NJ, Kent, England UFC Ltd, Manchester M15 6SY, Lancs, England UFC Ltd Manchester Lancs England M15 6SY nchester M15 6SY, Lancs, England
Titolo Testata:
BIOCATALYSIS AND BIOTRANSFORMATION
fascicolo: 1, volume: 19, anno: 2001,
pagine: 69 - 83
SICI:
1024-2422(2001)19:1<69:TSOTGM>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
GLYCOSIDE SYNTHESIS; ACID;
Keywords:
glucuronide; biocatalysis; imidate method;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
17
Recensione:
Indirizzi per estratti:
Indirizzo: Webster, R Pfizer Ltd, Cent Res, Dept Drug Metab, Sandwich CT13 9NJ, Kent,England Pfizer Ltd Sandwich Kent England CT13 9NJ 3 9NJ, Kent, England
Citazione:
R. Webster et al., "The synthesis of the glucuronide metabolite of UK-157,147 using immobilised uridine 5 '-diphosphoglucuronyl transferase and traditional organic chemistry techniques (imidate method)", BIOCATAL B, 19(1), 2001, pp. 69-83

Abstract

UK-157,147 (systematic name (3S,4R)-[6-(3-hydroxyphenyl)sulfonyl]-2,2,3-trimethyl-4-(2- methyl-3-oxo-2,3-dihydropyridazin-6-yloxy)-3-chromanol), a potent potassium channel opener designed for rapid systemic clearance, is metabolised in vivo to a glucuronide metabolite. A standard of this metaboliteof UK-157,147 was required for biological testing to confirm the absence of pharmacological activity and assay development. The glucuronide conjugateof UK-157,147 was initially synthesised using a bioreactor containing immobilised microsomes as a source of uridine 5'-diphosphoglucuronyl transferase (E.C.2.4.1.17). At a later date, larger amounts of the glucuronide metabolite were synthesised by traditional organic chemistry techniques using theimidate method. The identity of the chemically and biocatalytically produced glucuronide conjugate sample was proven by LC-MS and LC-NMR-MS.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 16:23:22