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Titolo:
NOVEL PLASMA KALLIKREIN INHIBITORS OF THE BENZAMIDINE TYPE
Autore:
STURZEBECHER J; PRASA D; WIKSTROM P; VIEWEG H;
Indirizzi:
UNIV JENA,ZENTRUM VASK BIOL & MED,INST BIOCHEM,NORDHAUSER STR 78 D-99089 ERFURT GERMANY PENTAPHARM LTD CH-4002 BASEL SWITZERLAND
Titolo Testata:
Brazilian journal of medical and biological research
fascicolo: 8, volume: 27, anno: 1994,
pagine: 1929 - 1934
SICI:
0100-879X(1994)27:8<1929:NPKIOT>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
THROMBIN;
Keywords:
PLASMA KALLIKREIN; INHIBITORS; BENZAMIDINES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
5
Recensione:
Indirizzi per estratti:
Citazione:
J. Sturzebecher et al., "NOVEL PLASMA KALLIKREIN INHIBITORS OF THE BENZAMIDINE TYPE", Brazilian journal of medical and biological research, 27(8), 1994, pp. 1929-1934

Abstract

Besides guanidino compounds and amines structurally related to arginine and lysine, compounds with an amidino moiety are inhibitors of trypsin-like enzymes. However, in most cases ordinary benzamidine derivatives are not selective inhibitors. Relatively selective inhibitors of some enzymes were found among amino acids containing a benzamidine moiety at the side chain. For example, derivatives of phenyl-alpha-aminobutyric acid with one or two amidino moieties such as the 4'-amidinoanilide of N alpha-[4-amidinophenylsulfonyl]-phenyl-alpha-acid are potent and selective inhibitors of plasma kallikrein (K-i = 0.15 mu M). UsingN alpha-arylsulfonylated 3-amidinophenylalanine as the key building block, novel inhibitors of plasma kallikrein were developed. Several esters and amides of the nipecotic acid derivative were synthesized which inhibit plasma kallikrein competitively with K-i values between 0.1 and 1.0 mu M. The compounds prolonged aPTT in micromolar concentration, indicating an inhibition of the intrinsic coagulation pathway.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/07/20 alle ore 02:21:01