title: Novel inhibitors of plasminogen activator inhibitor-1: development of new templates from diketopiperazines.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, Xenova Ltd., Slough, Berkshire, UK. shouming_wang@xenova.co.uk
authors.forename: Shouming
authors.initials: S
authors.lastname: Wang
authors.forename: Julian
authors.initials: J
authors.lastname: Golec
authors.forename: Warren
authors.initials: W
authors.lastname: Miller
authors.forename: Sandra
authors.initials: S
authors.lastname: Milutinovic
authors.forename: Adrian
authors.initials: A
authors.lastname: Folkes
authors.forename: Susannah
authors.initials: S
authors.lastname: Williams
authors.forename: Teresa
authors.initials: T
authors.lastname: Brooks
authors.forename: Kevin
authors.initials: K
authors.lastname: Hardman
authors.forename: Peter
authors.initials: P
authors.lastname: Charlton
authors.forename: Stephen
authors.initials: S
authors.lastname: Wren
authors.forename: John
authors.initials: J
authors.lastname: Spencer
mesh_terms: 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
chemical_list: D054659:Diketopiperazines; D010879:Piperazines; D017395:Plasminogen Activator Inhibitor 1