In this note, the synthesis and structure-activity relationships of a new series of 2R,2'R/2S,2'S and 2R,2'S-meso 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinones] are described. Antiinflammatory activity was investigated by the carrageenin-induced paw edema test and analgesic activity by acetic acid writhing and hot plate tests in rats. All compounds displayed ulcerogenic effects and acute toxicity much lower than indomethacin and phenylbutazone. Meso isomers (b) showed better pharmacological profiles than corresponding racemates (a). Methoxy substitution patterns of the aryls on stereogenic carbons are generally the most favorable on the pharmacological profile.

Synthesis and antiinflammatory, analgesic activity of 3,3’-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10.

VIGORITA, Maria;OTTANA', Rosaria;MACCARI, Rosanna;TROVATO, Ada;MONFORTE, Maria Teresa;TAVIANO, Maria Fernanda
2001

Abstract

In this note, the synthesis and structure-activity relationships of a new series of 2R,2'R/2S,2'S and 2R,2'S-meso 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinones] are described. Antiinflammatory activity was investigated by the carrageenin-induced paw edema test and analgesic activity by acetic acid writhing and hot plate tests in rats. All compounds displayed ulcerogenic effects and acute toxicity much lower than indomethacin and phenylbutazone. Meso isomers (b) showed better pharmacological profiles than corresponding racemates (a). Methoxy substitution patterns of the aryls on stereogenic carbons are generally the most favorable on the pharmacological profile.
File in questo prodotto:
Non ci sono file associati a questo prodotto.
Pubblicazioni consigliate

Caricamento pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11570/1910586
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? 8
  • Scopus 155
  • ???jsp.display-item.citation.isi??? 137
social impact