Design, synthesis, and pharmacological evaluation of some 2-[4-morpholino]-3-aryl-5-substituted thiophenes as novel anti-inflammatory agents: generation of a novel anti-inflammatory pharmacophore

Bioorganic & Medicinal Chemistry
Ajay D PillaiVasudevan Sudarsanam

Abstract

Compounds incorporating a thiophene moiety, a pi excess five membered heterocycle, have attracted a great deal of research interest owing to the therapeutic utility of the template as useful drug molecular scaffolding. Recently we reported the anti-inflammatory activity profile exhibited by two thiophene analogs, AP84 and AP82 in acute and chronic models of inflammation. The good activity profile exhibited by AP84, a 3-(substituted aryl)-2-(4-morpholino)-5-heteroaryl substituted analog of thiophene, in the formalin induced rat paw edema chronic model as compared to a weak activity in acute carrageenin induced rat paw edema, and the slightly better protection exhibited in the acute model by AP82 (27%), the 5-aroyl analog provided an impetus for a proper exploration of their structural types. In this paper we report the synthesis and pharmacological evaluation of some novel, 2-(4-morpholino)-3-(substituted aryl)-5-substituted thiophenes, as possible anti-inflammatory leads. The 3-(4-chlorophenyl)-2-(4-morpholino) thiophene analogs AP49, AP158, and AP88 provided a protection of 20%, 23%, and 20%, respectively, when screened for anti-inflammatory activity in carrageenin induced rat paw edema, an acute in vivo model, comparable to t...Continue Reading

Citations

Aug 20, 2011·The Journal of Organic Chemistry·Ganesh Chandra NandiMaya Shankar Singh
Jan 25, 2012·International Journal of Molecular Sciences·Juan C Garro MartinezEduardo A Castro
May 28, 2009·Journal of Enzyme Inhibition and Medicinal Chemistry·Ritesh N SharmaShyam S Pancholi
Jan 13, 2011·Organic & Biomolecular Chemistry·Daniela A BarancelliGilson Zeni

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