European Journal of Medicinal Chemistry p. 569 - 579 (1990)
Update date:2022-07-30
Topics:
Previtera
Vigorita
Basile
Fenech
Trovato
Occhiuto
Monforte
Barbera
A class of anti-inflammatory, analgesic and histamine H1- and H2-receptor antagonists the 2,2'-dihetero-arylbisthiazolidinones and their 1,1'-disulfones, obtained as [RR, SS] and [RS, SR] isomers, is described. The heteroaryl substitution at 2 and 2' carbons generally improves the pharmacological activities with respect to those of the previously studied 2,2'-diaryl analogues. In particular the 2,2'-dithienyl derivatives exhibit analgesic properties and, as [RS, SR] isomers 6b, 11b, 12b H2-histamine receptor antagonism as well. The most effective acute anti-inflammatory agents appear to be the 2,2'-di(3-pyridyl) compounds 8a, 8b, 14a, 14b which also display analgesic activity. Moreover, an H1-histamine receptor antagonism is almost selectively exerted by the 2,2'-di(2-pyridyl) derivatives 7a, 7b, 13a, 13b. The relationships between the assessed activities and the chirality and/or the sulfur oxidation state of the molecules are discussed. The anti-cancer potential was also evaluated against P 388 murine lymphocytic leukemia; however, the results were not significant.
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