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Titolo:
Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors
Autore:
Kokko, FP; Arrigoni, CE; Dix, TA;
Indirizzi:
Med Univ S Carolina, Dept Pharmaceut Sci, Charleston, SC 29425 USA Med Univ S Carolina Charleston SC USA 29425 Sci, Charleston, SC 29425 USA
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 14, volume: 11, anno: 2001,
pagine: 1947 - 1950
SICI:
0960-894X(20010723)11:14<1947:SEIBSO>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
RECEPTOR-BINDING AFFINITIES; ASYMMETRIC-SYNTHESIS; AMINO-ACIDS; ACTIVE-SITE; DESIGN; POTENT; BENZAMIDINE; DERIVATIVES; COMPLEX; UTILIZE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
23
Recensione:
Indirizzi per estratti:
Indirizzo: Dix, TA Med Univ S Carolina, Dept Pharmaceut Sci, POB 250140, Charleston, SC 29425USA Med Univ S Carolina POB 250140 Charleston SC USA 29425 SC 29425USA
Citazione:
F.P. Kokko et al., "Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors", BIOORG MED, 11(14), 2001, pp. 1947-1950

Abstract

Seven non-natural analogues of arginine and lysine have been substituted in an established arginine-based thrombin inhibitor. Four of the new compounds exhibited significant thrombin inhibition (K-i's 0.53-3.95 muM) and weresubsequently tested for selectivity against trypsin. The two best compounds gave selectivity ratios of 962 and 525 (trypsin/thrombin), improving uponthe parent compound. (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 00:38:01