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1: Org Biomol Chem. 2004 Jun 7;2(11):1633-42. Epub 2004 May 12. Links

Design, synthesis and biological activity of a targeted library of potential tryptase inhibitors.

García M, del Rio X, Silvestre S, Rubiralta M, Lozoya E, Segarra V, Fernández D, Miralpeix M, Aparici M, Diez A.

Laboratori de Química Orgànica, Facultat de Farmàcia, Universitat de Barcelona, Spain.

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.

PMID: 15162216 [PubMed - indexed for MEDLINE]