摘要：Novel primaquine conjugates with non-steroidal anti- -inlammatory drugs (PQ-NSAIDs,4a-h) were prepared,fully chemically characterized and screened for radical scavenging and antioxidant activities.The synthetic procedure leading to twin drugs 4a-h involved two steps: i) preparation of NSAID benzotriazolides 3a-h from the corresponding NSAID (ibuprofen,ketoprofen,fenoprofen,ketoprofen hydroxy and methylene analogues,diclofenac or indomethacin) and benzotriazole carboxylic acid chloride (BtCOCl,1),ii) reaction of intermediates 3a-h with PQ.The prepared PQ-NSAIDs exerted moderate activities in the DPPH free radical test and b-carotene-linoleic acid assay.Moreover,ketoprofen derivatives 4d and 4b demonstrated a notable Fe2+ chelating ability as well.On the other hand,negligible antiproliferative and antituberculotic effects of conjugates 4a-h were observed.
