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Titolo:
Development of potent and selective plasmin and plasma kallikrein inhibitors and studies on the structure-activity relationship
Autore:
Okada, Y; Tsuda, Y; Tada, M; Wanaka, K; Okamoto, U; 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 Gakuin Univ, High Technol Res Ctr, Nishi Ku, Kobe, Hyogo 6512180, Japan Kobe 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 pan 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: 12, volume: 48, anno: 2000,
pagine: 1964 - 1972
SICI:
0009-2363(200012)48:12<1964:DOPASP>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
CENTER-DIRECTED PLASMIN; HAGEMAN-FACTOR; ACTIVATION; COAGULATION; ELASTASE;
Keywords:
plasmin inhibitor; plasma kallikrein inhibitor; selectivity; structure-activity relationship;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
30
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 potent and selective plasmin and plasma kallikrein inhibitors and studies on the structure-activity relationship", CHEM PHARM, 48(12), 2000, pp. 1964-1972

Abstract

Based on structure-activity relationship studies, we designed and synthesized plasmin (PL) and plasma kallikrein (PK) inhibitors. Trans-(4-aminomethylcyclohesanecarbonyl)-Tyr( O-Pic)-octylamide inhibited PL, PK, urokinase (UK) and thrombin (TH) with IC50 values of 0.53, 30, 5.3 and >400 muM, respectively: Trans-(4-amino methylcyclohesanecarbonyl)-Tyr(O-2-Pyrim)-4-carboxyanilide inhibited PL, PK, UK and TH with IC50 values of 36, 0.56, 430 and >1000 muM, respectively.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/09/20 alle ore 11:42:50