The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold |
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Affiliation: | 1. College of Chemistry and Life Sciences, Zhejiang Normal University, Jinhua 321004, China;2. Centre for Synthesis and Chemical Biology, UCD School of Chemistry and Chemical Biology, University College Dublin, Belfield, Dublin 4, Ireland |
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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. |
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