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Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators

机译:苯并咪唑衍生物作为有效的AMP激活的蛋白激酶激活剂的合成和生物学评估

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摘要

Design, synthesis and structure-activity relationships of beU:/AP/DTD501/BMC/4818nzimidazole derivatives as activators of the AMP-activated protein kinase (AMPK) are presented in this paper. AMPK is the central component of a protein kinase cascade that plays a key role in the regulation of energy balance. Once activated, AMPK initiates a series of responses that are aimed at restoring the energy balance of the cell and recent studies have indicated that AMPK plays an important role in regulation of the whole-body energy metabolism. The following study based on the lead compound S27847 involved modification of three regions of this compound. Preliminary structure-activity relationships are being described.
机译:本文介绍了beU:/ AP / DTD501 / BMC / 4818nzimidazole衍生物作为AMP激活的蛋白激酶(AMPK)的激活剂的设计,合成和构效关系。 AMPK是蛋白激酶级联反应的核心成分,在调节能量平衡中起关键作用。激活后,AMPK会启动一系列旨在恢复细胞能量平衡的反应,最近的研究表明AMPK在调节全身能量代谢中起着重要作用。基于先导化合物S27847的以下研究涉及该化合物三个区域的修饰。正在描述初步的结构-活性关系。

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