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Titolo:
Development of plasmin-selective inhibitors and studies of their structure-activity relationship
Autore:
Okada, Y; Matsumoto, Y; Tsuda, Y; Tada, M; Wanaka, K; Hijikata-Okunomiya, A; Okamoto, S;
Indirizzi:
Kobe Gakuin Univ, Fac Pharmaceut Sci, Nishi Ku, Kobe, Hyogo 6512180, JapanKobe Gakuin Univ Kobe Hyogo Japan 6512180 Ku, Kobe, Hyogo 6512180, Japan Kobe Res Projects Thrombosis & Haemostasis, Tarumi Ku, Kobe, Hyogo 6550033, Japan Kobe Res Projects Thrombosis & Haemostasis Kobe Hyogo Japan 6550033 Japan Kobe Univ, Sch Med, Fac Hlth Sci, Suma Ku, Kobe, Hyogo 6540142, Japan KobeUniv Kobe Hyogo Japan 6540142 i, Suma Ku, Kobe, Hyogo 6540142, Japan
Titolo Testata:
CHEMICAL & PHARMACEUTICAL BULLETIN
fascicolo: 2, volume: 48, anno: 2000,
pagine: 184 - 193
SICI:
0009-2363(200002)48:2<184:DOPIAS>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
KALLIKREIN; SYSTEM;
Keywords:
plasmin inhibitor; selectivity; structure-activity relationship; N-(trans-4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-BrZ)-octylamide;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
19
Recensione:
Indirizzi per estratti:
Indirizzo: Okada, Y Kobe Gakuin Univ, Fac Pharmaceut Sci, Nishi Ku, Kobe, Hyogo 6512180, Japan Kobe Gakuin Univ Kobe Hyogo Japan 6512180 , Hyogo 6512180, Japan
Citazione:
Y. Okada et al., "Development of plasmin-selective inhibitors and studies of their structure-activity relationship", CHEM PHARM, 48(2), 2000, pp. 184-193

Abstract

Various compounds were synthesized by combining three components at positions P1, P-1' and P-2'. Of these, N-(trans-4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-bromobenzyloxycarbonyl)-octylamide inhibited plasmin selectively with IC50 values of 0.80 and 0.23 mu M towards S-2251 and fibrin, respectively This compound also inhibited plasma kallikrein, urokinase, thrombin and trypsin with IC50 values of 10, >50, >50 and 1.6 mu M, respectively.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/09/20 alle ore 12:19:51