Structure–activity relationship of human glutaminyl cyclase inhibitors having an N-(5-methyl-1H-imidazol-1-yl) propyl thiourea template

…, DW Nam, H Song, I Mook-Jung, J Lee, J Lee

文献索引：Lee, Jeewoo; Tran, Phuong-Thao; Hoang, Van-Hai; Thorat, Shivaji A.; Kim, Sung Eun; Ann, Jihyae; Chang, Yu Jin; Nam, Dong Woo; Song, Hyundong; Mook-Jung, Inhee; Lee, Jiyoun Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 13 p. 3821 - 3830

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被引用次数: 5

摘要

In an effort to design inhibitors of human glutaminyl cyclase (QC), we have synthesized a library of N-aryl N-(5-methyl-1H-imidazol-1-yl) propyl thioureas and investigated the contribution of the aryl region of these compounds to their structure–activity relationships as cyclase inhibitors. Our design was guided by the proposed binding mode of the preferred substrate for the cyclase. In this series, compound 52 was identified as the most potent QC ...