申请人:Merck & Co., Inc.
公开号:US05629343A1
公开(公告)日:1997-05-13
Novel N-(mercaptoacyl)peptidyl compounds are useful as inhibitors of matrix metalloendoproteinases which degrade major components of articular cartilage and basement membranes causing degenerative diseases such as arthritis, periodontal disease, corneal ulceration, are described. For example, N-(2-thiomethyl-4-phenyl-butanoyl)-L-leucinamide was prepared and its inhibitory activity against stromelysin was tested in vitro.
新型N-(巯基酰基)肽类化合物可作为基质金属内皮蛋白酶的抑制剂,这些酶会降解关节软骨和基底膜的主要成分,导致退行性疾病,如关节炎、牙周病、角膜溃疡等。例如,制备了N-(2-硫甲基-4-苯基-丁酰基)-L-亮氨酰胺,并在体外测试了其对溶解酶的抑制活性。