Michaelides M R, Dellaria J F, Gong J, Holms J H, Bouska J J, Stacey J, Wada C K, Heyman H R, Curtin M L, Guo Y, Goodfellow C L, Elmore I B, Albert D H, Magoc T J, Marcotte P A, Morgan D W, Davidsen S K
Cancer Research Area, Abbott Laboratories, Dept. 47J, Bldg. AP10, 100 Abbott Park Road, Abbott Park, IL 60064, USA.
Bioorg Med Chem Lett. 2001 Jun 18;11(12):1553-6. doi: 10.1016/s0960-894x(01)00031-2.
A novel series of biaryl ether reverse hydroxamate MMP inhibitors has been developed. These compounds are potent MMP-2 inhibitors with limited activity against MMP-1. Select members of this series exhibit excellent pharmacokinetic properties with long elimination half-lives (7 h) and high oral bioavailability (100%).
已开发出一系列新型的联芳基醚反向异羟肟酸酯基质金属蛋白酶(MMP)抑制剂。这些化合物是强效的MMP-2抑制剂,对MMP-1的活性有限。该系列中的特定成员具有出色的药代动力学性质,消除半衰期长(7小时)且口服生物利用度高(100%)。