IDENTIFICATION OF A POTENT ANALOG OF NAZUMAMIDE-A THROUGH ITERATION OF COMBINATORIAL TETRAPEPTIDE LIBRARIES

Authors
KUNDU B BAUSER M BETSCHINGER J KRAAS W JUNG G
Citation
B. Kundu et al., IDENTIFICATION OF A POTENT ANALOG OF NAZUMAMIDE-A THROUGH ITERATION OF COMBINATORIAL TETRAPEPTIDE LIBRARIES, Bioorganic & medicinal chemistry letters, 8(13), 1998, pp. 1669-1672
Citations number
7
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
13
Year of publication
1998
Pages
1669 - 1672
Database
ISI
SICI code
0960-894X(1998)8:13<1669:IOAPAO>2.0.ZU;2-N
Abstract
Five sets of N-acylated tetrapeptide libraries and sublibraries relate d to Nazumamide A have been prepared using 25 natural and unnatural am ino acids. They were evaluated in antithrombin assay, in order to quan tify inhibition at each step of the tetrapeptide sublibrary iteration. The studies led to the identification of droxybenzoyl-lysyl-isoleucyl -phenylalanyl-arginine as a novel inhibitor of thrombin and was found to be at least 25 times more potent than the natural tetrapeptide 2,5- benzoyl-arginyl-prolyl-isoleucy-alpha-aminobutyric acid (NAZA). (C) 1 998 Elsevier Science Ltd. All rights reserved.