合成和评估可被人类羧基酯酶代谢活化的具有二酯结构的吲哚美辛原药

IF 1.3 4区 医学 Q4 PHARMACOLOGY & PHARMACY Xenobiotica Pub Date : 2023-12-23 DOI:10.1080/00498254.2023.2298270
Daisuke Takani, Masato Takahashi, Masakiyo Hosokawa
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引用次数: 0

摘要

人们对羧基酯酶(CES)进行了广泛的研究,其中大部分是以单酯结构为底物。我们研究了吲哚美辛二酯原药与代谢活化之间的关系。
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Synthesis and evaluation of indomethacin prodrugs with a diester structure that are metabolically activated by human carboxylesterases
Carboxylesterase (CES) has been studied extensively, mostly with substrates in the monoester structures. We investigated the relationship between indomethacin diester prodrugs and metabolic activat...
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来源期刊
Xenobiotica
Xenobiotica 医学-毒理学
CiteScore
3.80
自引率
5.60%
发文量
96
审稿时长
2 months
期刊介绍: Xenobiotica covers seven main areas, including:General Xenobiochemistry, including in vitro studies concerned with the metabolism, disposition and excretion of drugs, and other xenobiotics, as well as the structure, function and regulation of associated enzymesClinical Pharmacokinetics and Metabolism, covering the pharmacokinetics and absorption, distribution, metabolism and excretion of drugs and other xenobiotics in manAnimal Pharmacokinetics and Metabolism, covering the pharmacokinetics, and absorption, distribution, metabolism and excretion of drugs and other xenobiotics in animalsPharmacogenetics, defined as the identification and functional characterisation of polymorphic genes that encode xenobiotic metabolising enzymes and transporters that may result in altered enzymatic, cellular and clinical responses to xenobioticsMolecular Toxicology, concerning the mechanisms of toxicity and the study of toxicology of xenobiotics at the molecular levelXenobiotic Transporters, concerned with all aspects of the carrier proteins involved in the movement of xenobiotics into and out of cells, and their impact on pharmacokinetic behaviour in animals and manTopics in Xenobiochemistry, in the form of reviews and commentaries are primarily intended to be a critical analysis of the issue, wherein the author offers opinions on the relevance of data or of a particular experimental approach or methodology
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