Synthesis and biological activities of 2,3-dihydro-1,3,4-oxadiazole compounds and its derivatives as potential activator of ryanodine receptors

ZhouY.; WangB.; DiF.; XiongL.; YangN.; LiY.; LiZ.

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Synthesis and biological activities of 2,3-dihydro-1,3,4-oxadiazole compounds and its derivatives as potential activator of ryanodine receptors

机译：2,3-二氢-1,3,4-二氧化氮化合物及其衍生物的合成及生物活性作为瑞尼诺受体的潜在活化剂

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摘要

A series of novel 2,3-dihydro-1,3,4-oxadiazoles containing N-pyridylpyrazole carboxamides moieties were obtained by applying a new synthetic route. Their insecticidal tests against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) indicated that most of the compounds showed moderate to excellent activities at the testing concentrations. In particular, compound 6a showed 40% larvicidal activities against oriental armyworm at 1 mg/L, while 7a against diamondback was 100% at 0.01 mg/L. Calcium imaging results demonstrated that 6a, 6d and 7a stimulated a transient elevation in [Ca2+]i in the absence of external calcium after the central neurons dye loading with fluo-3 AM, implying that these novel compounds were potential activators of the ligand-gated calcium channel on the endoplasmic reticulum.

机译：通过施加新的合成途径获得含有N-吡啶基吡唑羧酰胺部分的一系列新的2,3-二氢-1,3,4-二氧化氮。他们对东方武器（神话中的杀虫剂）和Diamondback Moth（Plutella Xylostella）的杀虫试验表明，大多数化合物在测试浓度下显示出中等至优异的活性。特别地，化合物6a显示了1mg / L的东方羊毛的40％幼稚活性，而7A抗蛋白返回为100％，0.01mg / L。钙成像结果证明，6A，6D和7A在中央神经元染料染料染料染料染料染料染料染料后施用瞬态升高，这意味着这些新化合物是配体门控的潜在活化剂内质网上的钙通道。

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《Bioorganic and Medicinal Chemistry Letters》 |2014年第10期|共5页
作者
ZhouY.; WangB.; DiF.; XiongL.; YangN.; LiY.; LiZ.;
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作者单位

State Key Laboratory of Elemento-Organic Chemistry Institute of Elemento-Organic Chemistry Nankai;

State Key Laboratory of Elemento-Organic Chemistry Institute of Elemento-Organic Chemistry Nankai;

State Key Laboratory of Elemento-Organic Chemistry Institute of Elemento-Organic Chemistry Nankai;

State Key Laboratory of Elemento-Organic Chemistry Institute of Elemento-Organic Chemistry Nankai;

State Key Laboratory of Elemento-Organic Chemistry Institute of Elemento-Organic Chemistry Nankai;

State Key Laboratory of Elemento-Organic Chemistry Institute of Elemento-Organic Chemistry Nankai;

State Key Laboratory of Elemento-Organic Chemistry Institute of Elemento-Organic Chemistry Nankai;

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正文语种 eng
中图分类药学;
关键词
2; 3-Dihydro-1; 3; 4-oxadiazoles; Calcium channel; Insecticidal activity;

机译：2;3-二氢-1;3;4-氧基Zoles;钙通道;杀虫活性;

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1. Synthesis and biological activities of 2,3-dihydro-1,3,4-oxadiazole compounds and its derivatives as potential activator of ryanodine receptors [J] . ZhouY., WangB., DiF., Bioorganic and Medicinal Chemistry Letters . 2014,第10期

机译：2,3-二氢-1,3,4-二氧化氮化合物及其衍生物的合成及生物活性作为瑞尼诺受体的潜在活化剂
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Synthesis and biological activities of 2,3-dihydro-1,3,4-oxadiazole compounds and its derivatives as potential activator of ryanodine receptors

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