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Synthesis and evaluation of the anti-inflammatory activity of some 2-(Trimethoxyphenyl)-4-R1-5-R2-Thiazoles

This paper is available in a repository.
This paper is available in a repository.

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Abstract

There is an increasing need to obtain new anti-inflammatory molecules that act either as COX-2 selective inhibitors or as iNOS inhibitors. To that effect, we synthesized some 2-(trimethoxyphenyl)-4-R1-5-R2-thiazoles and evaluated their anti-inflammatory properties. Experimental. The main synthesis route involved the Hantzsch condensation of the 3,4,5-trimethoxy-benzothioamide with various α-halo-ketones. For all synthesized compounds, the anti-inflammatory activity was evaluated in vivo on an experimental acute inflammation at rats thought the acute phase bone marrow response, phagocytic capacity, and nitro-oxidative stress status. Results. A total of 13 new compounds were synthesized and all of them have various degrees of anti-inflammatory activity. All tested compounds reduced the acute phase bone marrow response, the phagocytic capacity and the nitro-oxidative stress. Conclusions. Two of the compounds had a more potent action than meloxicam in all studied areas.