DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NOVEL 1,3-INDANEDIONE DERIVATIVES

In quest of elucidating the diverse pharmacological properties of 1,3-indanedione derivatives, we have synthesized a new series of 1,3-indanedione derivatives via Knovevanegal condensation, by condensing with the different aldehydes (Nitro benzalyhade) to form a styrylated indane dione leading to the formation of different Schiff base. The structures of compounds were characterized by 1H and 13C NMR, FT-IR and Mass spectral analysis. The newly synthesized compounds are evaluated for their antioxidant (NO and DPPH scavenging, and inhibition of lipid peroxidation), antimicrobial/antifungal, and anti-inflammatory activities. Compounds with phenolic group as the terminal substitution or meta- and para- di-substitutions are reported with superior antimicrobial, antifungal and anti-inflammatory activities. Compound 10 reported highest antimicrobial and antifungal activities and moderate antioxidant activity. Anti-inflammatory activity of compound 10 is statistically similar at 50 mg/kg dose with celecoxib (20 mg/kg). Molecular docking studies against COX2 enzyme were performed and reported similar observations and provided deeper understanding of the ligand conformations in the protein environment. Keywords: Indanedione, antibacterial agents, anti-oxidative, anti-inflammatory activity, molecular docking