Bioorganic & Medicinal Chemistry Letters 2005-03-15

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

Index: Bioorg. Med. Chem. Lett. 15 , 1659-64, (2005)

Full Text: HTML

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.