Chemical Informatics

Design, Synthesis and Stability Studies of Mutual Prodrugs of NSAID's

Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen and indomethacin have been conjugated with naturally occurring and synthetic phenolic and alcoholic antioxidants with the objective of obtaining NSAIDsantioxidant prodrugs as gastrosparing NSAIDs with improving therapeutic efficacy by masking of carboxylic group chemically. Promoieties like vanilline, and chalcone were selected with the aim of getting synergistic effect and antioxidant property. In silico prediction of solubility and partition coefficient was performed using calculated physicochemical parameters. All the prodrugs were found to be highly stable at acidic pH while undergoes hydrolysis at neutral and alkaline pH as indicated by their t1/2 values. Synthesized prodrug derivatives showed increased anti-inflammatory activity that might be attributed to synergistic effect as ibuprofen and indomethacin conjugates to antioxidants that are natural analgesics.

Author(s):

Prasanna Datar, Tejashree Shendge

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