A prolonged increase in pro-inflammatory cytokines, TNF-α and IL-6 occurs in inflammatory diseases. Although cinnoline belongs to a family of fairly well known heterocycles, the interest in the study of its derivatives continues. Cinnoline compounds demonstrate interesting bioactivity and many research papers have discussed the biological property, structureactivity relationship, and applications in medicinal science. A new series of substituted Cinnoline derivatives condensed with Thiophene moieties (12a-j) were synthesized and their anti-inflammatory was evaluated. The anti-inflammatory activity was assessed by rat paw edema method. The pharmacological screening showed that many of these obtained compounds have significant anti-inflammatory activity, comparable to the standard drug (phenylbutazone). The compound 12DSDi produces maximum anti-inflammatory activity compared to other tested compound.

In medicinal chemistry nitrogen containing heterocycles are the most important compounds which show various biological activities. The cinnoline are nitrogenous derivatives and found to elicit many pharmacological actions like anti-hypertensive, antithrombotic, antihistamine, antileukemic, CNS activity, anti tumor, antibacterial and antisecretory activity. We planned to synthesis new series of substituted Cinnoline derivatives, and evaluated for antibacterial, antifungal and anti-inflammatory activity. The Cinnoline moiety substituted with different substituents condensed with Pyrazole, Piperazine, Imidazole, Furan and Thiophene moieties separately. The antibacterial and antifungal activities of synthesized compounds were determined by disc diffusion method. The anti-inflammatory activity of synthesized compounds was assessed by rat paw edema method. The synthesized compound exhibited moderate to good antibacterial, antifungal and anti-inflammatory activity. The substituted Cinnoline Piperazine series and Cinnoline thiophene series compound exhibited maximum antibacterial activity and antifungal activity, respectively. The substituted Cinnoline Imidazole series revealed potent anti-inflammatory activity. Further investigations are required to find out possible mechanism of action.

No abstract

No abstract