Imaki K, Okada T, Nakayama Y, Nagao Y, Kobayashi K, Sakai Y, Mohri T, Amino T, Nakai H, Kawamura M
Department of Medicinal Chemistry, Minase Research Institute, Ono Pharmaceutical Co., Ltd., Osaka, Japan.
Bioorg Med Chem. 1996 Dec;4(12):2115-34. doi: 10.1016/s0968-0896(96)00216-7.
A novel series of pivaloyloxy benzene derivatives has been identified as potent and selective human neutrophil elastase (HNE) inhibitors. Convergent syntheses were developed in order to identify the inhibitors which are intravenously effective in an animal model. A compound of particular interest is the sulfonanilide-containing analogues. Structure-activity relationships are discussed. Structural requirements for metabolic stabilization are also discussed.
一系列新型的特戊酰氧基苯衍生物已被鉴定为强效且具有选择性的人中性粒细胞弹性蛋白酶（HNE）抑制剂。为了鉴定在动物模型中静脉给药有效的抑制剂，开展了汇聚合成研究。一种特别受关注的化合物是含磺酰苯胺的类似物。文中讨论了构效关系。还讨论了代谢稳定性的结构要求。
