A novel series of novobiocin analogues has been synthesised by removing the
lipophilic aryl chain in novobiocin and introducing an amino substituent.
The structural modifications have been dictated by the control of lipophili
city and the dissociation constant of the resulting compounds. Antibacteria
l activity of the new coumarin derivatives could be correlated with the amo
unt of uncharged form in physiological conditions. (C) 2001 Elsevier Scienc
e Ltd. All rights reserved.