14741285 |
Ye B, Chou YL, Karanjawala R, Lee W, Lu SF, Shaw KJ, Jones S, Lentz D, Liang A, Tseng JL, Wu Q, Zhao Z: Synthesis and biological evaluation of piperazine-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1). Bioorg Med Chem Lett. 2004 Feb 9;14(3):761-5. Compound 2 was identified by high throughput screening as a novel PAI-1 inhibitor. Systematic optimization of the A, B, and C segments of 2 resulted in the identification of a more potent compound 39 with good oral bioavailability. The synthesis and SAR data are presented in this report. |
82(1,1,1,2) |