- Etodolac, a novel antiinflammatory agent. The syntheses and biological evaluation of its metabolites
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The syntheses of five metabolites of the antiinflammatory drug etodolac (1,8-diethyl-1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acid) are described, viz. 6-hydroxyetodolac, N-methyletodolac, 4-ureidoetodolac, 8-(1'-hydroxy)etodolac, and 4-oxoetodolac. These syntheses were used to confirm the identities of the metabolites. The metabolites themselves, as well as the previously reported metabolite 7-hydroxyetodolac, were tested in a rat adjuvant edema model and in vitro for their capacity to block prostaglandin production in chondrocyte cells. All either were inactive or possessed only marginal activity. The isolation of N-methyletodolac and 4-oxoetodolac from human and rat urine, respectively, is also described.
- Humber,Ferdinandi,Demerson,Ahmed,Shah,Mobilio,Sabatucci,De Lange,Labbadia,Hughes,DeVirgilio,Neuman,Chau,Weichman
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p. 1712 - 1719
(2007/10/02)
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- Substituted 1,3,4,9-tetrahydropyrano(3,4-b)indole-1-acetic acids
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Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1 and 4. The nucleus may be optionally substituted at position 8. The derivatives are useful anti-inflammatory and a
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