DeVries V G, Bloom J D, Dutia M D, Katocs A S, Largis E E
Medical Research Division, American Cyanamid Company, Lederle Laboratories, Pearl River, New York 10965.
J Med Chem. 1989 Oct;32(10):2318-25. doi: 10.1021/jm00130a016.
The discovery that a series of N,N-dialkyl-N'-arylureas were inhibitors of the ACAT enzyme has led to a structure-activity study involving the systematic modification of three sites of the urea backbone. This study culminated in the selection of N'-(2,4-dimethylphenyl)-N-benzyl-N-n-butylurea (115) for more extensive biological evaluation. ACAT inhibitors are seen as potentially beneficial agents against hypercholesterolemia and atherosclerosis.
一系列N，N-二烷基-N'-芳基脲是酰基辅酶A：胆固醇酰基转移酶（ACAT）的抑制剂，这一发现引发了一项构效关系研究，该研究涉及对脲骨架三个位点的系统修饰。这项研究最终选定了N'-(2,4-二甲基苯基)-N-苄基-N-正丁基脲（115）进行更广泛的生物学评估。ACAT抑制剂被视为对抗高胆固醇血症和动脉粥样硬化的潜在有益药物。
