Combinatorial approaches towards the discovery of new tryptase inhibitors

Montserrat del Fresno; Dolors Fernández-Forner; Montserrat Miralpeix; Victor Segarra; Hamish Ryder; Miriam Royo; Fernando Albericio

doi:10.1016/j.bmcl.2005.01.048

Combinatorial approaches towards the discovery of new tryptase inhibitors

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1659-64. doi: 10.1016/j.bmcl.2005.01.048.

Authors

Montserrat del Fresno¹, Dolors Fernández-Forner, Montserrat Miralpeix, Victor Segarra, Hamish Ryder, Miriam Royo, Fernando Albericio

Affiliation

¹ Department of Organic Chemistry, University of Barcelona, Martí i Franquès, 1-11, 08028 Barcelona, Spain.

PMID: 15745817
DOI: 10.1016/j.bmcl.2005.01.048

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Combinatorial Chemistry Techniques / methods*
Models, Chemical
Molecular Structure
Piperazines / chemical synthesis
Piperazines / chemistry
Piperazines / pharmacology
Serine Endopeptidases / chemistry*
Serine Endopeptidases / metabolism
Serine Proteinase Inhibitors / chemical synthesis
Serine Proteinase Inhibitors / chemistry
Structure-Activity Relationship
Tryptases

Substances

Piperazines
Serine Proteinase Inhibitors
Serine Endopeptidases
Tryptases