Naslov
Primaquine-NSAID twin drugs: Synthesis, radical scavenging, antioxidant and Fe2+

Autori
Rajić, Zrinka ; Zovko, Končić Marijana ; Miloloža, Kristina ; Perković, Ivana ; Butula, Ivan ; Bucar, Franz ; Zorc, Branka

Izvornik
Acta pharmaceutica (1330-0075) 60 (2010), 3; 325-337

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
primaquine ; NSAID ; twin drug ; conjugate ; radical scavenging ; antioxidant activity ; chelating ability

Sažetak
Novel primaquine conjugates with non-steroidal anti-inflammatory 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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija

POVEZANOST RADA