SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF OPTICALLY-ACTIVE XYBENZYLAMINO)-2-HYDROXYPROPOXY]-2(1H)-QUINOLINONE (OPC-18790)

Authors
FUJIOKA T TERAMOTO S TSUJIMI S TAKEMOTO K MORI T HOSOKAWA T SUMIDA T TOMINAGA M YABUUCHI Y
Citation
T. Fujioka et al., SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF OPTICALLY-ACTIVE XYBENZYLAMINO)-2-HYDROXYPROPOXY]-2(1H)-QUINOLINONE (OPC-18790), Chemical and Pharmaceutical Bulletin, 44(8), 1996, pp. 1596-1598
Citations number
7
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Chemical and Pharmaceutical Bulletin → ACNP
ISSN journal
00092363
Volume
44
Issue
8
Year of publication
1996
Pages
1596 - 1598
Database
ISI
SICI code
0009-2363(1996)44:8<1596:SABOOX>2.0.ZU;2-8
Abstract
The enantiomers of xybenzylamino)-2-hydroxypropoxy]-2(1H)-quinolinone (OPC-18790), a novel cardiotonic agent, were synthesized and evaluated for positive inotropic activity. The key intermediates, 2,3-epoxyprop oxy derivatives, were obtained by the alkylation of 6-hydroxy-2(1H)-qu inolinone with optically active epichlorohydrin and subsequent ring cl osure. In an in vitro study, the (R)-(+)-isomer was about id-fold more potent than the (S)-(-)-isomer.