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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and blood glucose lowering effect of novel pyridazinone substituted benzenesulfonylurea derivatives.
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Synthesis and blood glucose lowering effect of novel pyridazinone substituted benzenesulfonylurea derivatives.

机译：新型哒嗪酮取代的苯磺酰脲衍生物的合成及降血糖作用。

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摘要

Fifteen novel pyridazinone substituted benzenesulfonylurea derivatives (3a-o) were synthesized from corresponding sulfonamides derivatives via novel carbamates (2a-e). These were characterized by elemental analysis and various spectroscopic methods viz. IR, (1)H NMR, (13)C NMR and MS. Blood sugar lowering effect of thirteen (3a-c, 3e, 3g-o) sulfonylurea derivatives at the dose of 20 mg/kg (p.o.) were assessed using glucose tolerance test in normal and NIDDM (n2-STZ) rat models. All compounds except 3c, 3e and 3o almost completely prevented the rise of blood glucose of NIDDM rats as compared with NIDDM control. While compounds 3c and 3o showed more than 50% prevention in the rise of blood glucose levels. In glucose-fed normal rats these compounds at the same dose except 3e significantly prevented the rise of blood glucose (more than 50%) when compared with control of glucose-fed normal rats. From the results, novel compounds (3a-c, 3g-n) exhibited considerably potent blood glucose lowering activity and may be used as lead compounds for developing new antidiabetic drugs. Some structure-activity relationship was observed while varying nature of 'Ar' and 'R'.
机译：通过新的氨基甲酸酯（2a-e）由相应的磺酰胺衍生物合成了十五种新的哒嗪酮取代的苯磺酰脲衍生物（3a-o）。这些通过元素分析和各种光谱方法表征。 IR，（1）H NMR，（13）C NMR和MS。使用葡萄糖耐量试验在正常和NIDDM（n2-STZ）大鼠模型中评估了13种（3a-c，3e，3g-o）磺酰脲衍生物在20 mg / kg（p.o.）剂量下的降血糖作用。与NIDDM对照组相比，除3c，3e和3o外的所有化合物几乎完全阻止了NIDDM大鼠的血糖升高。而化合物3c和3o显示出超过50％的预防可防止血糖水平升高。在葡萄糖喂养的正常大鼠中，与对照的葡萄糖喂养的正常大鼠相比，这些化合物以相同的剂量（3e除外）显着阻止了血糖的升高（超过50％）。从结果来看，新化合物（3a-c，3g-n）表现出相当强的降血糖活性，可以用作开发新的抗糖尿病药物的先导化合物。在改变“ Ar”和“ R”的性质时观察到一些结构-活性关系。

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