A study of the effects of substituents on the selectivity of the binding of N-arylaminomethylene malonate inhibitors to DHODH.

ID: ALA1159041

Journal: Bioorg Med Chem Lett

Title: A study of the effects of substituents on the selectivity of the binding of N-arylaminomethylene malonate inhibitors to DHODH.

Authors: Cowen D, Bedingfield P, McConkey GA, Fishwick CW, Johnson AP.

Abstract: A series of mono- and di-substituted N-arylaminomethylene malonates have been used to probe the potential of utilizing additional H-bonding contacts in the ubiquinone binding channel, for selective inhibition between either human or Plasmodium DHODH. Altered 'head' group functionalities have been utilized in order to probe the role of specific functionalities within the inhibitors in terms of enzyme affinity and selectivity.

CiteXplore: 20034791

DOI: 10.1016/j.bmcl.2009.11.079

Patent ID: ┄