New isoxazole derivatives designed as nicotinic acetylcholine receptor ligand candidates.

Silva NildaM; Tributino JorgeL M; Miranda AnaL P; Barreiro EliezerJ; Fraga CarlosA M

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New isoxazole derivatives designed as nicotinic acetylcholine receptor ligand candidates.

机译：被设计为烟碱乙酰胆碱受体配体候选物的新异恶唑衍生物。

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In this work we report the synthesis and evaluation of the analgesic properties of new isosteric heterocyclic derivatives, presenting the isoxazole nucleus, designed as nicotinic acetylcholine receptor ligand candidates, analogues to alkaloid epibatidine. Compound 2-(3-methyl-5-isoxazolyl)pyridine (3) presented the best analgesic profile of this series in hot plate test, which was partially prevented by pretreatment with nicotinic receptor antagonist mecamylamine.

机译：在这项工作中，我们报告了新的等规杂环衍生物的镇痛特性的合成和评估，提出了异恶唑核，被设计为烟碱乙酰胆碱受体配体候选物，类似于生物碱依法巴定。化合物2-（3-甲基-5-异恶唑基）吡啶（3）在热板试验中表现出该系列的最佳镇痛作用，但通过烟碱样受体拮抗剂美卡明胺预处理可部分阻止这种镇痛作用。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2002年第2期|共8页
作者
Silva NildaM; Tributino JorgeL M; Miranda AnaL P; Barreiro EliezerJ; Fraga CarlosA M;
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正文语种 eng
中图分类医药、卫生;
关键词
Analgesics; Isoxazoles; Nicotinic Antagonists; Receptors; Nicotinic; Ligands; 镇痛药; 异恶唑类; 烟碱拮抗剂; 受体; 烟碱;

机译：Analgesics;Isoxazoles;Nicotinic Antagonists;Receptors;Nicotinic;Ligands;镇痛药;异恶唑类;烟碱拮抗剂;受体;烟碱;

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1. New isoxazole derivatives designed as nicotinic acetylcholine receptor ligand candidates. [J] . Silva NildaM, Tributino JorgeL M, Miranda AnaL P, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2002,第2期

机译：被设计为烟碱乙酰胆碱受体配体候选物的新异恶唑衍生物。
2. Design of alpha 7 nicotinic acetylcholine receptor ligands in quinuclidine, tropane and quinazoline series. Chemistry, molecular modeling, radiochemistry, in vitro and in rats evaluations of a [F-18] quinuclidine derivative [J] . Pin Frederic, Vercouillie Johnny, Ouach Aziz, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2014,第Null期

机译：奎尼丁，托烷和喹唑啉系列中α7烟碱型乙酰胆碱受体配体的设计。化学，分子模型，放射化学，[F-18]喹核苷衍生物的体外和大鼠评价
3. Design and synthesis of isoxazole containing bioisosteres of epibatidine as potent nicotinic acetylcholine receptor agonists. [J] . Singh S, Avor KS, Pouw B, Chemical and Pharmaceutical Bulletin . 1999,第10期

机译：设计和合成含有依巴替丁的生物等位基因异恶唑作为有效的烟碱乙酰胆碱受体激动剂。
4. Progress in Brown Planthopper Nicotinic Acetylcholine Receptors and Possible Roles in Insecticides Design [C] . Liu Zewen 第三届“农药与环境安全”国际学术研讨会暨第七届“植物化学保护和全球法律一体化”国际研讨会（3rd I . 2007

机译：褐飞虱烟碱型乙酰胆碱受体的研究进展及其在杀虫剂设计中的作用
5. Modulation of nicotinic receptors by an allosteric ligand assessed using fast jumps in acetylcholine. [D] . Hirt, Spencer L. 2016

机译：使用乙酰胆碱的快速跳跃评估变构配体对烟碱样受体的调节。
6. Docking studies of benzylidene anabaseine interactions with α7 nicotinic acetylcholine receptor (nAChR) and acetylcholine binding proteins (AChBPs): Application to the design of related α7 selective ligands [O] . David C. Kombo, Anatoly Mazurov, Kartik Tallapragada, -1

机译：与α7烟碱乙酰胆碱受体（NACHR）和乙酰胆碱结合蛋白（ACHBPS）相互作用的对接研究（ACHBPS）：应用于相关α7选择性配体的设计
7. Insights into the Structural Determinants Required for High-Affinity Binding of Chiral Cyclopropane-Containing Ligands to α4β2-Nicotinic Acetylcholine Receptors: An Integrated Approach to Behaviorally Active Nicotinic Ligands [O] . Zhang, Han-Kun, Eaton, J Brek, Yu, Li-Fang, 2012

机译：深入了解手性含环丙烷的配体与α4β2-烟碱乙酰胆碱受体高亲和力结合所需的结构决定因素：行为活性烟碱配体的综合方法。

New isoxazole derivatives designed as nicotinic acetylcholine receptor ligand candidates.

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