title: Combinatorial approaches towards the discovery of new tryptase inhibitors.
abstract: The synthesis and evaluation as tryptase inhibitors of a library of 2,5-diketopiperazine derivatives containing guanidine or amidine functional groups is reported. Among the compounds evaluated, derivatives 6{CG4-CG8} and 6{CG4-CG9} are the most active compounds and have marked selectivity towards tryptase in front of trypsin.
authors.affiliation: Department of Organic Chemistry, University of Barcelona, Martí i Franquès, 1-11, 08028 Barcelona, Spain.
authors.forename: Montserrat
authors.initials: M
authors.lastname: del Fresno
authors.forename: Dolors
authors.initials: D
authors.lastname: Fernández-Forner
authors.forename: Montserrat
authors.initials: M
authors.lastname: Miralpeix
authors.forename: Victor
authors.initials: V
authors.lastname: Segarra
authors.forename: Hamish
authors.initials: H
authors.lastname: Ryder
authors.forename: Miriam
authors.initials: M
authors.lastname: Royo
authors.forename: Fernando
authors.initials: F
authors.lastname: Albericio
mesh_terms: D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D008956:Models, Chemical; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D012697:Serine Endopeptidases / Q000737:chemistry* / Q000378:metabolism; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D013329:Structure-Activity Relationship; D053802:Tryptases
chemical_list: D010879:Piperazines; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases