Sulfonamides as multifunctional agents for Alzheimer's disease
Sulfonamides as multifunctional agents for Alzheimer's disease
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DOI：
10.1016/j.bmcl.2014.12.006
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发表时间：
2015-02-01
影响因子：
2.7
通讯作者：
Toeroek, Marianna
中科院分区：
文献类型：
--
作者：
Bag, Seema;Tulsan, Rekha;Toeroek, Marianna
设计并合成了具有扩展线性结构的基于磺酰胺接头的抑制剂，目的是产生针对阿尔茨海默病（AD）病理学中涉及的几个过程的多功能剂。评估了化合物在抑制Ab自组装（原纤维和寡聚体形成）、调节胆碱酯酶（AChE、BuChE）活性和清除自由基方面的效力。几个化合物表现出有前途的抗体自组装和胆碱酯酶抑制和平行，表现出良好的自由基清除性能。本研究中描述的支架的研究导致鉴定出三种化合物（14、19和26）作为用于AD的多功能候选药物的进一步设计的有希望的先导物。(C)2014爱思唯尔有限公司版权所有。
Sulfonamide linker-based inhibitors with extended linear structure were designed and synthesized with the aim of producing multifunctional agents against several processes involved in the pathology of Alzheimer's disease (AD). The potency of the compounds were assessed in the inhibition of Ab self-assembly (fibril and oligomer formation), in modulating cholinesterase (AChE, BuChE) activity, and scavenging free radicals. Several compounds exhibited promising Ab self-assembly and cholinesterase inhibition and in parallel, showed good free radical scavenging properties. The investigation of the scaffold described in this study resulted in the identification of three compounds (14, 19 and 26) as promising leads for the further design of multifunctional drug candidates for AD. (C) 2014 Elsevier Ltd. All rights reserved.