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SYNTHESIS AND ANTI-DIABETIC ACTIVITY OF SOME ARYLOXYPROPANOLAMINE DERIVATIVES

机译:一些芳氧基丙醇胺衍生物的合成与抗糖尿病活性

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Aryloxypropanolamine plays an important role in several biological activities. It shows multiple actions such as |3-blocking, anxiolytic, antihypertensive and inhibition of cytochrome p450. A series of ten aryloxypropanolamine derivatives 6a-6j were synthesized and evaluated for anti-diabetic activity. Two compounds 6b to 6g have shown good anti-diabetic activity. All synthesized compounds (6a-6j) were evaluated for their anti-diabetic activity in STZ induced diabetes model of Wistar rats. Approximately 100 million people worldwide suffer from type II diabetes (NIDDM), which is characterized by hyperglycemia due to excessive hepatic production of glucose. Noninsulin dependent Diabetes mellitus(NIDDM type II diabetes) is chronic metabolic disease characterized by insulin resistance hyperglycemia. The term diabetes mellitus describes a metabolic disorder of multiple an etiologies characterized by chronic hyperglycemia with disturbances of carbohydrate, fat and protein metabolism resulting from defects in insulin secretion, insulin action or both. The aryloxypropanolamines were first described as beta 3 adrenergic receptor agonist in the mid1980s. Later on several pharmaceutical industries are engaged in developing potent selective beta 3 adrenergic receptor agonist for the treatment of type II diabetes and obesity. Aryloxypropanolamines are now a days playing a very important role as an anti-diabetic agents as well as anti-obesity agent, anti-hypertensive, anti-convulsants and in cardiovascular diseases.
机译:芳氧基丙二醇胺在几种生物活动中起着重要作用。它显示了多种作用,例如| 3-抗障碍,抗抑郁,抗高血压和抑制细胞色素P450。合成了一系列十种芳氧基丙醇胺衍生物6a-6j,并评估抗糖尿病活性。两种化合物6B至6G显示出良好的抗糖尿病活性。评价所有合成的化合物(6A-6J)在STZ诱导的Wistar大鼠患有糖尿病模型中进行抗糖尿病活性。全球约有100万人患有II型糖尿病(NIDDM),其特征是由于葡萄糖的过度肝脏生产引起的高血糖。非胰岛素依赖性糖尿病(Niddm II型糖尿病)是慢性代谢疾病,其特征在于胰岛素抵抗高血糖。术语术语Mellitus描述了多种病因的代谢障碍,其特征在于慢性高血糖,其具有由胰岛素分泌,胰岛素作用或两者缺陷导致的碳水化合物,脂肪和蛋白质代谢的紊乱。芳氧基丙二醇胺首先在1980年代中期被描述为β3肾上腺素能受体激动剂。后来在几种制药行业开始开发有效的选择性β3肾上腺素能受体激动剂,用于治疗II型糖尿病和肥胖症。芳基氧基丙醇胺现在是一种非常重要的作用,作为抗糖尿病药剂以及抗肥胖剂,抗高血压,抗痉挛剂和心血管疾病。

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