Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents

A series of pyrazolo[4,3-c]cinnoline derivatives was synthesized, characterized and evaluated for anti-inflammatory and antibacterial activity. Test compounds that exhibited good anti-inflammatory activity were further screened for their ulcerogenic and lipid peroxidation activity. Compounds 4d and 4l showed promising anti-inflammatory activity with reduced ulcerogenic and lipid peroxidation activity when compared to naproxen. Docking results of these two compounds with COX-2 (PDB ID: 1CX2) also exhibited a strong binding profile. Among the test derivatives, compound 4i displayed significant antibacterial property against gram-negative (Escherichia coli and Pseudomonas aeruginosa) and gram-positive (Staphylococcus aureus) bacteria. However, compound 4b emerged as the best dual anti-inflammatory–antibacterial agent in the present study. [Display omitted] ► A series of pyrazolo[4,3-c]cinnoline derivatives were synthesized. ► Characterized by IR, 1H NMR, 13C NMR, and DART-MASS technique. ► Anti-inflammatory, ulcerogenic, lipid peroxidation, COX-2 inhibition and antibacterial studies were performed. ► Compounds 4d and 4l showed excellent protection against inflammation. ► Compound 4b emerged as a potential dual anti-inflammatory–antibacterial agent.