SYNTHESIS AND CALCIUM ANTAGONISTIC ACTIVITY OF A SERIES OF DIETHYL BENZOFURYL, BENZOTHIENYL AND BENZOGAMMAPYRONYL BENZYLPHOSPHONATES

Authors
BAZIARDMOUYSSET G TCHANI GW STIGLIANI JL PAYARD M BONNAFOUS R TISNEVERSAILLES J
Citation
G. Baziardmouysset et al., SYNTHESIS AND CALCIUM ANTAGONISTIC ACTIVITY OF A SERIES OF DIETHYL BENZOFURYL, BENZOTHIENYL AND BENZOGAMMAPYRONYL BENZYLPHOSPHONATES, European journal of medicinal chemistry, 28(7-8), 1993, pp. 539-546
Citations number
32
Categorie Soggetti
Chemistry Medicinal
Journal title
European journal of medicinal chemistry → ACNP
ISSN journal
02235234
Volume
28
Issue
7-8
Year of publication
1993
Pages
539 - 546
Database
ISI
SICI code
0223-5234(1993)28:7-8<539:SACAAO>2.0.ZU;2-0
Abstract
In this work we present about 15 original heterocyclic diethyl benzylp hosphonate analogues of fostedil, in which we have varied the nature o f the heterocycle, the substituents or the phosphonic group, or even t he position of this latter. Three diethyl 4-(2-benzofuryl) benzyl phos phonates exhibited slightly higher calcium antagonism than the control . Solely substitution with a fluorine atom was able to maintain activi ty, whereas the other modifications always decreased it.