Combinatorial approaches towards the discovery of new tryptase inhibitors.
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.
del Fresno
Montserrat
M
Department of Organic Chemistry, University of Barcelona, Martí i Franquès, 1-11, 08028 Barcelona, Spain.
Fernández-Forner
Dolors
D
Miralpeix
Montserrat
M
Segarra
Victor
V
Ryder
Hamish
H
Royo
Miriam
M
Albericio
Fernando
F
D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D008956:Models, Chemical; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D012697:Serine Endopeptidases / Q000737:chemistry* / Q000378:metabolism; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D013329:Structure-Activity Relationship; D053802:Tryptases
D010879:Piperazines; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases