Design, synthesis and SAR analysis of potent BACE1 inhibitors: Possible lead drug candidates for Alzheimer's disease

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• 作者：Hamadeh Tarazi^a ; ^b ; Raed Abu Odeh^b ; ^c ; Raed Al-Qawasmeh^d ; Imad Abu Yousef^e ; Wolfgang Voelter^f ; Taleb H. Al-Tel^a ; ^b ; ^{taltal@sharjah.ac.ae}
• 关键词：β-secretase inhibitors ; Alzheimer's disease ; Transition state mimics ; Structure-based drug design ; Structure activity relationship ; Isophthalic acid derivatives ; Molecular modeling
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：1213-1224
• 全文大小：1980 K
• 卷排序：125

文摘

Four new series of isophthalic acid derivatives clubbed with Indolyl-Imidazole derivatives were synthesized. Some of the synthesized compounds exhibited potent activity against BACE1. A QSAR model of the synthesized motifs was developed using QSARINS software.