Combinatorial approaches towards the discovery of new tryptase inhibitors
Montserrat del Fresno1, Dolors Fernández-Forner, Montserrat Miralpeix
1Department of Organic Chemistry, University of Barcelona, Martí i Franquès, 1-11, 08028 Barcelona, Spain.
Bioorganic & Medicinal Chemistry Letters
|March 5, 2005
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.
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