The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold.

Autor: Tullis JS; Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700Mason-Montgomery Rd, Mason, OH 45040, USA., Laufersweiler MJ, VanRens JC, Natchus MG, Bookland RG, Almstead NG, Pikul S, De B, Hsieh LC, Janusz MJ, Branch TM, Peng SX, Jin YY, Hudlicky T, Oppong K
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Aug 06; Vol. 11 (15), pp. 1975-9.
DOI: 10.1016/s0960-894x(01)00371-7
Abstrakt: 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.
Databáze: MEDLINE