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-恶二唑化合物及其衍生物作为ryanodine受体的潜在活化剂的合成及生物学活性

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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：通过采用新的合成途径，获得了一系列含有N-吡啶基吡唑羧酰胺部分的新颖的2,3-二氢-1,3,4-恶二唑。他们对东方粘虫（Mythimna separata）和小菜蛾（Plutella xylostella）的杀虫测试表明，大多数化合物在测试浓度下均表现出中等至出色的活性。特别是，化合物1a在1 mg / L时对东方粘虫的杀幼虫活性为40％，而化合物7a在0.01 mg / L时对小菜蛾的杀幼虫活性为100％。钙成像结果表明，在中央神经元染料上加入fluo-3 AM后，在不存在外部钙的情况下，6a，6d和7a刺激了[Ca2 +] i的瞬时升高，这暗示这些新化合物是配体门控的潜在激活剂。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
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ZhouY.; WangB.; DiF.; XiongL.; YangN.; LiY.; LiZ.;
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正文语种 eng
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2; 3-Dihydro-1; 3; 4-oxadiazoles; Calcium channel; Insecticidal activity;

机译：2;3-二氢-1;3;4-恶二唑;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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机译：肼 - 腙及其相应的3-乙酰基-2,5-二取代的2,3-二氢-1,3,4-恶二唑对埃及伊蚊的叮咬威慑和杀虫活性

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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