Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1355620 | Bioorganic Chemistry | 2015 | 13 Pages |
•New quinolines incorporated pyrazoles were synthesized.•Screening of anti-inflammatory, analgesic, and ulcerogenic activities were performed for the synthesized compounds.•Molecular modeling study was performed for compounds (5–11).
In continuation of our study of novel quinolines with anti-inflammatory activity using the Pfitzinger reaction, several new quinoline derivatives were synthesized and tested for their anti-inflammatory and ulcerogenic effect. A docking study on the COX-2 binding pocket was carried out for the target compounds to rationalize the possible selectivity of them against COX-2 enzyme. The most active compounds (5a, 8a and 11a) were found to be superior to celecoxib. Compound 11a demonstrated the highest anti-inflammatory activity as well as the best binding profiles into the COX-2 binding site. Moreover, compounds 9c, 9e, 10a and 11a were devoid of ulcerogenic activity.
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