In pursuing our search on anti-inflammatory dl and meso 3,3′-di[1,3-thiazolidine-4-one] compounds, two series of derivatives have been prepared by modifying the substitution pattern at positions 1 and 2 of the heterocyclic rings and by introducing an ethylene chain between nitrogen atoms. The anti-inflammatory activity of these compounds has been preliminarily assayed against carrageenin-induced rat paw edema: those proven to be active were also tested for analgesic, anti-pyretic and anti-histamine properties. As a whole, the obtained results suggest that some of the new derivatives possess significant anti-histamine activity. The meso forms generally are more active than dl ones in agreement with the previously emphasized SAR of the chiral systems under study.
3,3' - Di 1,3-Thiazolidine-one system. II. Antiinflammatory and anti-histaminic properties in new substituted derivatives.
OCCHIUTO, Francesco;CIRCOSTA, Clara;
1987-01-01
Abstract
In pursuing our search on anti-inflammatory dl and meso 3,3′-di[1,3-thiazolidine-4-one] compounds, two series of derivatives have been prepared by modifying the substitution pattern at positions 1 and 2 of the heterocyclic rings and by introducing an ethylene chain between nitrogen atoms. The anti-inflammatory activity of these compounds has been preliminarily assayed against carrageenin-induced rat paw edema: those proven to be active were also tested for analgesic, anti-pyretic and anti-histamine properties. As a whole, the obtained results suggest that some of the new derivatives possess significant anti-histamine activity. The meso forms generally are more active than dl ones in agreement with the previously emphasized SAR of the chiral systems under study.Pubblicazioni consigliate
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