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Titolo:
Design, synthesis and pharmacological evaluation of 3-benzylazetidine-2-one-based human chymase inhibitors
Autore:
Aoyama, Y; Uenaka, M; Kii, M; Tanaka, M; Konoike, T; Hayasaki-Kajiwara, Y; Naya, N; Nakajima, M;
Indirizzi:
Shionogi & Co Ltd, Shionogi Res Labs, Fukushima Ku, Osaka 5530002, Japan Shionogi & Co Ltd Osaka Japan 5530002 Fukushima Ku, Osaka 5530002, Japan Shionogi & Co Ltd, Shionogi Res Labs, Amagasaki, Hyogo 6600813, Japan Shionogi & Co Ltd Amagasaki Hyogo Japan 6600813 aki, Hyogo 6600813, Japan Shionogi & Co Ltd, Shionogi Res Labs, Osaka 5610825, Japan Shionogi & Co Ltd Osaka Japan 5610825 ogi Res Labs, Osaka 5610825, Japan
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 11, volume: 9, anno: 2001,
pagine: 3065 - 3075
SICI:
0968-0896(200111)9:11<3065:DSAPEO>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN-LEUKOCYTE ELASTASE; MAST-CELL CHYMASE; BETA-LACTAM INHIBITORS; II-FORMING CHYMASE; ESTERS; HEART; SPECIFICITY; EXPRESSION; ACTIVATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
30
Recensione:
Indirizzi per estratti:
Indirizzo: Aoyama, Y Shionogi & Co Ltd, Shionogi Res Labs, Fukushima Ku, Osaka 5530002, Japan Shionogi & Co Ltd Osaka Japan 5530002 Ku, Osaka 5530002, Japan
Citazione:
Y. Aoyama et al., "Design, synthesis and pharmacological evaluation of 3-benzylazetidine-2-one-based human chymase inhibitors", BIO MED CH, 9(11), 2001, pp. 3065-3075

Abstract

3-Benzylazetidine-2-one derivatives were designed and evaluated as a novelseries of chymase inhibitors. Structure-activity relationship studies of 3-benzylazetidine-2-ones led to compounds 23, which exhibited 3.1 nM inhibition of human chymase and enhancement of stability in human plasma (t(1/2) 6h). (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 04/04/20 alle ore 15:23:07