Potent and Selective Carboxylic Acid-Based Inhibitors of Matrix Metalloproteinases

Autor: Pikul, S., Ohler, N. E., Ciszewski, G., Laufersweiler, M. C., Almstead, N. G., De, B., Natchus, M. G., Hsieh, L. C., Janusz, M. J., Peng, S. X., Branch, T. M., King, S. L., Taiwo, Y. O., Mieling, G. E.
Zdroj: Journal of Medicinal Chemistry; August 2001, Vol. 44 Issue: 16 p2499-2502, 4p
Abstrakt: A novel series of carboxylic acids containing a substituted piperidine were synthesized and tested for inhibition of selected matrix metalloproteinases. Multiple analogues prepared based on this novel design were found to inhibit the target MMPs (MMP-2, -3, -8, -9, and -13) with unprecedented, low nanomolar potency while, at the same time, sparing MMP-1 and MMP-7. Solubility and plasma protein binding of several members of this new series of carboxylic acids were also investigated.
Databáze: Supplemental Index