Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin

• Published in: Journal of medicinal chemistry Vol. 30; no. 11; pp. 2051 - 2058
• Main Authors: Gillard, J. W, Belanger, P
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 01.11.1987; Amer Chemical Soc
• Subjects: Animals; Anti-Inflammatory Agents - chemical synthesis; Anti-Inflammatory Agents - pharmacology; Chemistry, Medicinal; Indomethacin - metabolism; Indomethacin - pharmacology; Life Sciences & Biomedicine; Pharmaceutical Preparations - chemical synthesis; Pharmacology & Pharmacy; Prodrugs - chemical synthesis; Prodrugs - pharmacology; Rats; Science & Technology; Species Specificity

Arylacetic acid antiinflammatory drugs can be metabolically produced by .beta.-oxidation of a 6-arylhex-5-enoic acid side chain. Such a mechanism provides an in vivo [mice and rats] sustained release of the active principle indomethacin from 6-[N-(p-chlorobenzoyl)-2-methylindol-3-yl]hex-5-enoic acid...