Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines.

@article{Natchus2000DevelopmentON,
  title={Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines.},
  author={Michael G. Natchus and Roger G Bookland and Biswanath De and Neil G. Almstead and Stanislaw Pikul and Michael J Janusz and Sandra A Heitmeyer and Erin B Hookfin and Lily C Hsieh and Martin E. Dowty and Charles R. Dietsch and Vikram Patel and S M Garver and Feng-lin Gu and Matthew E. Pokross and Glen Edward Mieling and Tracie R Baker and David J Foltz and Sean X. Peng and David M. Bornes and M J Strojnowski and Yetunde O Taiwo},
  journal={Journal of medicinal chemistry},
  year={2000},
  volume={43 26},
  pages={4948-63}
}
A series of hydroxamates was prepared from an aminoproline scaffold and tested for efficacy 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 47, display broad-spectrum activity with sub-nanomolar potency for some enzymes. Modifications of the P1' portion of the molecule played a key role in affecting both potency and selectivity within the MMP family. Longer-chain aliphatic… CONTINUE READING

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