Synthesis of New N‐Substituted 5‐Arylidene‐2, 4‐thiazolidinediones as Anti‐Inflammatory and Antimicrobial Agents. Issue 6 (13th May 2013)

• Record Type: Journal Article
• Authors: Nastasă, Cristina; Tiperciuc, Brînduşa; Pârvu, Alina; Duma, Mihaela; Ionuţ, Ioana; Oniga, Ovidiu
• Is Part Of: Archiv der Pharmazie. Volume 346:Issue 6(2013:Jun.)
• Page Start: 481
• Page End: 490
• Publication Date: 2013-05-13
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201300021
• Languages: English
• ISSNs: 0365-6233

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>A novel series of 5‐arylidene<bold>‐</bold>2, 4‐thiazolidinediones (TZDs) <bold>2a</bold>–<bold>p</bold> was synthesized from the condensation of 3‐((2‐phenylthiazol‐4‐yl)methyl)thiazolidine‐2, 4‐dione with different benzaldehyde derivatives. All the structures were confirmed by their spectral (IR, ¹H NMR, ¹³C NMR and mass) and elemental analytical data. The new molecules were evaluated <italic>in vivo</italic> as anti‐inflammatory agents in an acute experimental inflammation, evaluating the acute phase bone marrow response and phagocyte activity. All compounds, excepting one, reduced the absolute leukocytes count due to the lower neutrophil percentage. Phagocytary index was decreased by the same molecules, while only half of them reduced the phagocytary activity. The effect was superior to meloxicam, the reference anti‐inflammatory drug, for the majority of the TZD derivatives. The new molecules were also investigated for their antimicrobial properties on Gram‐positive and Gram‐negative bacteria and one fungal strain. Two compounds (<bold>2e</bold> and <bold>2n</bold>) manifested growth inhibition capacity on all the tested strains.</p> </abstract>