title: Design, synthesis and biological activity of a targeted library of potential tryptase inhibitors.
abstract: We have designed, synthesized, and tested two small collections of potential tryptase inhibitors. The first library consists of diversely N-substituted 3-aminopiperidin-2-ones 6, and the second (compounds 7) was prepared by dimerising compounds 6 through the 3-amino function using diverse carbon chains. We have established efficient routes for obtaining 6 both in solution and on solid supports. We have also compared the dimerisation on-resin and in solution. Four of the compounds showed a high degree of tryptase inhibition at 1 microM, but none surpassed the tryptase inhibition activity of BABIM.
authors.affiliation: Laboratori de Química Orgànica, Facultat de Farmàcia, Universitat de Barcelona, Spain.
authors.forename: Mónica
authors.initials: M
authors.lastname: García
authors.forename: Xavier
authors.initials: X
authors.lastname: del Rio
authors.forename: Sandra
authors.initials: S
authors.lastname: Silvestre
authors.forename: Mario
authors.initials: M
authors.lastname: Rubiralta
authors.forename: Estrella
authors.initials: E
authors.lastname: Lozoya
authors.forename: Victor
authors.initials: V
authors.lastname: Segarra
authors.forename: Dolors
authors.initials: D
authors.lastname: Fernández
authors.forename: Montserrat
authors.initials: M
authors.lastname: Miralpeix
authors.forename: Mònica
authors.initials: M
authors.lastname: Aparici
authors.forename: Anna
authors.initials: A
authors.lastname: Diez
mesh_terms: D019281:Dimerization; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D010881:Piperidones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D012697:Serine Endopeptidases; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D053802:Tryptases
chemical_list: C016997:3-aminopiperidine-2-one; D010881:Piperidones; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases