Discovery of novel series of 6-benzyl substituted 4-aminocarbonyl-1, 4-diazepane-2, 5-diones as human chymase inhibitors using structure-based drug design

T Tanaka, H Sugawara, H Maruoka, S Imajo…

文献索引：Tanaka, Taisaku; Sugawara, Hajime; Maruoka, Hiroshi; Imajo, Seiichi; Muto, Tsuyoshi Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 14 p. 4233 - 4249

全文：HTML全文

被引用次数: 3

摘要

A novel series of 6-benzyl substituted 4-aminocarbonyl-1, 4-diazepane-2, 5-diones were explored as human chymase inhibitors using structure-based drug design according to the X- ray cocrystal structure of chymase and compound 1. The optimization focused on the prime site led to the attainment of compounds that showed potent inhibitory activity, and among them, 18R shows a novel interaction mode.