Antiinflammatory And Analgesic Activities Of Two Dicyclic Analogues Of Acetaminophen And Its Regioisomer 3-Hydroxyacetanilide

K. lakovou; A. Varvaresou; G. Bruni; P. Massarelli; A. Vavayannis; M. Kazanis

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Antiinflammatory And Analgesic Activities Of Two Dicyclic Analogues Of Acetaminophen And Its Regioisomer 3-Hydroxyacetanilide

机译：对乙酰氨基酚的两个双环类似物及其区域异构体3-羟基乙酰苯胺的抗炎和镇痛作用

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Many of the nonsteroidal antiinflammatory drugs (NSAIDs) currently marketed produce severe gastrotoxic side effects. However, acetaminophen (4-hydroxyacetanili-de), which is devoid of gastrotoxicity, is associated with hepatotoxicity and nephrotoxicity.Hepatotoxicity and nephrotoxicity of acetaminophen in man and experimental animals have been attributed to metabolic conversion of the drug into a reactive intermediate by the cytochrome P450 dependent mixed function oxidase system [1]. N-acetyl-p-benzoquinoneimine (NAPQI) is the most likely structure for the ultimate reactive intermediate that depletes cellular glutathione (GSH) and covalently binds to tissue macromolecules [2, 3].

机译：当前市售的许多非甾体抗炎药（NSAID）都会产生严重的胃毒副作用。然而，对乙酰氨基酚（4-羟基对乙酰氨基酚）无胃毒性，与肝毒性和肾毒性有关。 P450依赖的混合功能氧化酶系统[1]。 N-乙酰基-对-苯并醌亚胺（NAPQI）是最终反应性中间体的最可能结构，其耗尽细胞谷胱甘肽（GSH）并与组织大分子共价结合[2，3]。

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《Pharmaceutical Chemistry Journal》 |2004年第5期|共4页
作者
K. lakovou; A. Varvaresou; G. Bruni; P. Massarelli; A. Vavayannis; M. Kazanis;
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正文语种 eng
中图分类药学;
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1. Antiinflammatory And Analgesic Activities Of Two Dicyclic Analogues Of Acetaminophen And Its Regioisomer 3-Hydroxyacetanilide [J] . K. lakovou, A. Varvaresou, G. Bruni, Pharmaceutical Chemistry Journal . 2004,第5期

机译：对乙酰氨基酚的两个双环类似物及其区域异构体3-羟基乙酰苯胺的抗炎和镇痛作用
2. Combining paracetamol (acetaminophen) with nonsteroidal antiinflammatory drugs: a qualitative systematic review of analgesic efficacy for acute postoperative pain. [J] . Ong CK, Seymour RA, Lirk P, Anesthesia and Analgesia: Journal of the International Anesthesia Research Society . 2010,第4期

机译：将对乙酰氨基酚（对乙酰氨基酚）与非甾体抗炎药合用：定性的系统评价，用于急性术后疼痛的镇痛效果。
3. Analgesic effects of nonsteroidal antiinflammatory drugs, acetaminophen, and morphine in a mouse model of bone cancer pain. [J] . Saito O, Aoe T, Yamamoto T Journal of anesthesia . 2005,第3期

机译：非甾体抗炎药，乙酰氨基酚和吗啡在骨癌疼痛小鼠模型中的镇痛作用。
4. Effects of Naloxone and JTC-801 on Analgesic Activity of Novel N/OFQ(1-13)NH2 Analogues [C] . Adriana I. Bocheva, Elena B. Dzhambazova, Petar T. Todorov American Peptide Symposium . 2011

机译：纳洛酮和JTC-801对新型Q（1-13）NH2类似物镇痛活性的影响
5. Improved extraction of acylated anthocyanins from purple sweet potato (Ipomoea batata) for enhanced antiinflammatory activity and their metabolite production during porcine fecal digestion [D] . Cipriano, Paula De Aguiar. 2016

机译：改进了从紫甘薯（Ipomoea batata）中提取酰化花色苷的方法，以增强猪粪便消化过程中的抗炎活性及其代谢产物的产生
6. p53 Contributes to Differentiating Gene Expression Following Exposure to Acetaminophen and Its Less Hepatotoxic Regioisomer Both In Vitro and In Vivo [O] . Brendan D Stamper, Michael L Garcia, Duy Q Nguyen, 2015

机译：p53有助于在暴露于对乙酰氨基酚及其肝脏毒性较低的区域异构体后体外和体内差异化基因表达。
7. A Combined Study Using Ligand-Based Design, Synthesis, and Pharmacological Evaluation of Analogues of the Acetaminophen Ortho-Regioisomer with Potent Analgesic Activity [O] . Queiroz, Luana M. D., Rocha, Josmar Rodrigues da, Leitão, Andrei, 2012

机译：结合使用基于配体的设计，合成和药理学评价对乙酰氨基酚邻位-区域异构体具有有效止痛活性的类似药物

Antiinflammatory And Analgesic Activities Of Two Dicyclic Analogues Of Acetaminophen And Its Regioisomer 3-Hydroxyacetanilide

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