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Abstract
Nineteen bisthiazoles were tested in order to assess their anti-inflammatory and antioxidant properties. First, we evaluated the in vitro direct antioxidant capacity of the bisthiazoles using the DPPH radical scavenging method. Then, the anti-inflammatory effect was tested in acute rat experimental inflammation by measuring the acute phase bone marrow response, the phagocytic capacity and the serum nitro-oxidative stress status. Although none of the substances showed significant direct antioxidant potential in the DPPH assay, most of them improved serum oxidative status, when administered to rats with inflammation. Four of the bisthiazoles proved to have good anti-inflammatory properties, similar or superior to that of equal doses meloxicam.
Highlights
Nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the most frequently used therapeutic classes of drugs
As a central moiety we focused on the bisthizole due to the presence of the thiazole ring in other NSAID and due to bioisosterism of the thiazole with the pyrazole or isoxazole ring
The direct antioxidant effect of the new bisthiazoles was determined in order to assess if an eventual anti-inflammatory effect through the reduction of the oxidative stress may be due to the direct radical scavenging ability
Summary
Nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the most frequently used therapeutic classes of drugs. Despite their large scale utilisation, many problems regarding their safety profile have been signalled over the years. We decided to focuse on 1,3-diaryl-heterocyclic systems as recent studies showed that molecules with 1,3-diaryl-heterocyclic structures are active as COX-2 inhibitors and may possess various central heterocyclic systems: pyrazole [11,12], triazole [13], tiazolidinedione [14]. Besides simultaneous inhibition of COX-2 and iNOS another potentially beneficial action in the treatment of inflammation could be the additional direct antioxidant effect of the molecule [18]. Using an acute rat experimental inflammation model we assessed the acute phase bone marrow response, the phagocytic capacity and the nitro-oxidative stress
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