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Background: 4-Aminoquinoline derivatives possess various potential biological properties such as anti-inflammatory and analgesic activity. The introduction of additional piperazine heterocyclic pharmacophoric moiety tends to exert profound influence in increasing the activity. The aim of the present work was to investigate the in-vitro and in-vivo anti-inflammatory activity as well as the peripheral and central analgesic activities of compound 1-(4-(7-chloroquinolin-4-yl)piperazin-1-yl)-2-(4-phenylpiperazin-1-yl)ethanone (5) in experimental models7-chloro-4-(piperazin-1-yl)quinoline derivatives 1-9 demonstrated significant inhibition of nitric oxide level in RAW 264.7 cells. Results: compound 5 demonstrated the highest NO inhibitory activity that was accompanied by inhibition of iNOS protein expression as well as decreased gene expression levels of inflammatory markers iNOS, COX2, IL-6, IL-1β, and TNF-α in RAW 264.7. Compound 5 revealed a potential peripheral analgesic effect through inhibition of abdominal writhing in mice treated with doses of 15mg/kg and 30 mg/kg and its effect was comparable to diclofenac sodium. Compound 5 possessed an analgesic activity starting from 15 min post administration and reached its peak at 45 min that was significantly higher than that of tramadol hydrochloride suggesting its potential as central analgesic agent (hot-plate test). Compound 5 showed percentage of inhibition of edema of 34, 50 and 64% at 1, 2, and 3 h respectively, post carrageenan challenge. This was accompanied by a significant decrease in serum NO and COX-2 levels. Conclusions: The remarkable anti-inflammatory and analgesic activities of compound 5 could be attributed to the advantageous introduction of the heterocyclic 7-chloro-4-(piperazin1-yl)quinoline scaffold incorporated with N-phenylpiperzine functional groups linked together with the ethanone pharmacophoric chain.

̒ulūm-i dārūyī

Anti-Inflammatory and Analgesic Activities of 7-Chloro-4-(Piperazin-1-yl) Quinoline Derivative Mediated by Suppression of InflammatoryMediators Expression in Both RAW 264.7 and Mouse Models