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Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Authors:Ye Bin  Bauer Shawn  Buckman Brad O  Ghannam Ameen  Griedel Brian D  Khim Seock-Kyu  Lee Wheeseong  Sacchi Karna L  Shaw Kenneth J  Liang Amy  Wu Qingyu  Zhao Zuchun
Affiliation:Discovery Research, Berlex Biosciences, 2600 Hilltop Drive, PO Box 4099, Richmond, CA 94804-0099, USA. bin_ye@berlex.com
Abstract:Compound 1 was identified by high throughput screening as a novel PAI-1 inhibitor. Optimization of the B and C-segments of 1 resulted in a series of structurally simplified compounds with improved potency. The synthesis and SAR data of these compounds are presented here.
Keywords:
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