GASTROPROTECTIVE EFFECT OF STEREOISOMERIC CIS-2-(1-PYRROLIDINYL) AND TRANS-2-(1-PYRROLIDINYL) AND 2-(1-PYRROLIDINYLMETHYL)CYCLOHEXYL ALKOXYCARBANILATES IN RATS

Citation
V. Nosalova et al., GASTROPROTECTIVE EFFECT OF STEREOISOMERIC CIS-2-(1-PYRROLIDINYL) AND TRANS-2-(1-PYRROLIDINYL) AND 2-(1-PYRROLIDINYLMETHYL)CYCLOHEXYL ALKOXYCARBANILATES IN RATS, Die Pharmazie, 52(12), 1997, pp. 950-952
Citations number
10
Categorie Soggetti
Pharmacology & Pharmacy","Chemistry Medicinal
Journal title
ISSN journal
00317144
Volume
52
Issue
12
Year of publication
1997
Pages
950 - 952
Database
ISI
SICI code
0031-7144(1997)52:12<950:GEOSCA>2.0.ZU;2-V
Abstract
The effect of cis-and trans-isomers of 2-(1-pyrrolidinyl) and of 2-(1- pyrrolidinylmethyl)cyclohexyl alkoxycarbanilates was tested in acute g astric injury induced by phenylbutazone and/or 96% ethanol administrat ion in rats. In both models a more pronounced antiulcer and gastroprot ective activity was observed after pretreatment with the trans-isomer of 2-(1-pyrrolidinyl)cyclohexyl ester of 3(n)-pentyloxycarbanilic acid . Its cis-isomer, by comparison, was less effective against ethanol-in duced gastric injury and failed to prevent the gastric damage induced by phenylbutazone. After introducing a methylene group into the hydrop hilic part of the molecule, there was a loss of sterospecific differen ce, with both stereoisomers exerting a similar gastroprotective activi ty.