Chemical synthesis of an indomethacin ester prodrug and its metabolic activation by human carboxylesterase 1

• Published in: Bioorganic & medicinal chemistry letters Vol. 28; no. 6; pp. 997 - 1000
• Main Authors: Takahashi, Masato, Ogawa, Tomohiro, Kashiwagi, Hiroshi, Fukushima, Fumiya, Yoshitsugu, Misaki, Haba, Masami, Hosokawa, Masakiyo
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 01.04.2018; Elsevier
• Subjects: Carboxylesterase; Chemistry; Chemistry, Medicinal; Chemistry, Organic; Chiral recognition; Indomethacin; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Physical Sciences; Prodrug; Science & Technology; Thioester; Indomethacin; Prodrug; Carboxylesterase; Thioester; Chiral recognition; SPECIFICITY; COCAINE; INTESTINE; ISOZYMES; HEROIN; AGENT; HUMAN LIVER; INHIBITORS; DERIVATIVES; BINDING

[Display omitted] It is necessary to consider the affinity of prodrugs for metabolic enzymes for efficient activation of the prodrugs in the body. Although many prodrugs have been synthesized with consideration of these chemical properties, there has been little study on the design of a structure wi...