Bioorganic & Medicinal Chemistry Letters 28 (2018) 997–1000 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl Chemical synthesis of an indomethacin ester prodrug and its metabolic activation by human carboxylesterase 1 Masato Takahashi , Tomohiro Ogawa, Hiroshi Kashiwagi, Fumiya Fukushima, Misaki Yoshitsugu, Masami Haba, Masakiyo Hosokawa Faculty of Pharmacy, Chiba Institute of Science, 15-8, Shiomi-cho, Choshi, Chiba 288-0025, Japan article i nfo abstract Article history: It is necessary to consider the afﬁnity of prodrugs for metabolic enzymes for efﬁcient activation of the Received 28 December 2017 prodrugs in the body. Although many prodrugs have been synthesized with consideration of these chem- Revised 16 February 2018 ical properties, there has been little study on the design of a structure with consideration of biological Accepted 16 February 2018 properties such as substrate recognition ability of metabolic enzymes. In this report, chemical synthesis Available online 21 February 2018 and evaluation of indomethacin prodrugs metabolically activated by human carboxylesterase 1 (hCES1) are described. The synthesized prodrugs were subjected to hydrolysis reactions in solutions of human Keywords: liver microsomes (HLM), human intestine microsomes (HIM) and hCES1, and the hydrolytic parameters Indomethacin were investigated to evaluate the hydrolytic rates of
Bioorganic & Medicinal Chemistry Letters – Elsevier
Published: Apr 1, 2018
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