Synthesis and Pharmacological Evaluation of Indanone Derivatives

Abstract

Derivatives of Isoxazole fused Indanones were synthesized from chalcone derivatives of indane-1,3-dione by condensation with hydroxyl amine hydrochloride. The synthesized compounds were confirmed by IR, 1H NMR and Mass spectral data. Synthesized derivatives were investigated for their pharmacological activity. Anti-inflammatory activity was carried out using carrageenan induced paw oedema method. The derivatives BD6 and BD7 showed moderate anti-inflammatory activity. Analgesic activity was carried out using hot plate method. The derivatives BD6 and BD7 showed good analgesic activity. Antibacterial and antifungal activity was carried out using cup plate method at 25, 50, 100 μg/mL. BD6, BD10 and BD11 showed good anti-bacterial and antifungal activity at 100 μg/mL. It was observed that the synthesized compounds possessing electron donating (-CH3, -OH) in phenyl ring exhibited good pharmacological activities when compared to that of other synthesized compounds. The effect of a number of functional group substitutions on pharmacological properties of the indanone molecular scaffold is examined through a detailed docking.