Campbell D A, Xiao X Y, Harris D, Ida S, Mortezaei R, Ngu K, Shi L, Tien D, Wang Y, Navre M, Patel D V, Sharr M A, DiJoseph J F, Killar L M, Leone C L, Levin J I, Skotnicki J S
Affymax Research Institute, Santa Clara, CA 95051, USA.
Bioorg Med Chem Lett. 1998 May 19;8(10):1157-62. doi: 10.1016/s0960-894x(98)00185-1.
A novel series of matrix metalloproteinase (MMP) inhibitors is described. Incorporation of a terminal alpha-mercaptoketone or alpha-mercaptoalcohol in the zinc binding domain of a series of inhibitors led to compounds exhibiting low nanomolar activity against collagenase-1 (MMP-1), stromelysin (MMP-3), and gelatinase-B (MMP-9).
描述了一系列新型的基质金属蛋白酶(MMP)抑制剂。在一系列抑制剂的锌结合结构域中引入末端α-巯基酮或α-巯基醇,得到了对胶原酶-1(MMP-1)、基质溶解素(MMP-3)和明胶酶-B(MMP-9)表现出低纳摩尔活性的化合物。