Novel inhibitors of plasminogen activator inhibitor-1: development of new templates from diketopiperazines.
Several isoquinoline-based templates were identified from the studies of the conformational effects of the diketopiperazine structures for PAI-1 inhibition. Moderate to good activity was retained with the elimination of unattractive characteristics in the diketopiperazine template.
Wang
Shouming
S
Department of Medicinal Chemistry, Xenova Ltd., Slough, Berkshire, UK. shouming_wang@xenova.co.uk
Golec
Julian
J
Miller
Warren
W
Milutinovic
Sandra
S
Folkes
Adrian
A
Williams
Susannah
S
Brooks
Teresa
T
Hardman
Kevin
K
Charlton
Peter
P
Wren
Stephen
S
Spencer
John
J
D054659:Diketopiperazines; D006801:Humans; D020128:Inhibitory Concentration 50; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D017395:Plasminogen Activator Inhibitor 1 / Q000737:chemistry*; D011485:Protein Binding; D013329:Structure-Activity Relationship
D054659:Diketopiperazines; D010879:Piperazines; D017395:Plasminogen Activator Inhibitor 1