SYNTHESES OF CYCLOPENTANE, CYCLOHEXENE AND OLEFIN OXAZOLES AS THROMBOXANE-A(2) ENDOPEROXIDE RECEPTOR ANTAGONISTS

Authors
DAS J HALL SE REID JA HAN WC HARRIS DN GOLDENBERG H MICHEL IM MONSHIZADEGAN H WEBB ML
Citation
J. Das et al., SYNTHESES OF CYCLOPENTANE, CYCLOHEXENE AND OLEFIN OXAZOLES AS THROMBOXANE-A(2) ENDOPEROXIDE RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 3(6), 1993, pp. 1267-1270
Citations number
11
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
6
Year of publication
1993
Pages
1267 - 1270
Database
ISI
SICI code
0960-894X(1993)3:6<1267:SOCCAO>2.0.ZU;2-O
Abstract
Synthesis and antiplatelet activity of a series of structurally simple thromboxane A2 receptor antagonists are described. The cis-cyclopenta ne analog (-)-1c was the most potent compound in this series with 150 and K(d) values of 15 nM and 4.3+/-0.0 nM, respectively. In radioligan d binding assay, trans-cyclopentane analog (-)-1d was the most potent ligand with a K(d) value of 0.5+/-0.3 nM.