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The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold
J S Tullis1, M J Laufersweiler, J C VanRens
1Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700Mason-Montgomery Rd, Mason, OH 45040, USA.
Bioorganic & Medicinal Chemistry Letters
|July 17, 2001
Abstract:
A series of carboxylic acids was prepared based on cyclohexylglycine scaffolds and tested for potency as matrix metalloproteinase (MMP) inhibitors. Detailed SAR for the series is reported for five enzymes within the MMP family, and a number of inhibitors such as compound 18 display low nanomolar potency for MMP-2 and MMP-13, while selectively sparing MMP-1 and MMP-7.