Many central nervous system (CNS) diseases such as Alzheimer’s disease (AD) have inflammatory pathology that is difficult to treat due to the limited number of anti-inflammatory drugs with sufficient brain bioavailability. N-Methyl-N-benzylamide derivatives could be utilized to shuttle drugs such as non-steroidal anti-inflammatory drugs (NSAIDs) across the blood-brain barrier (BBB) for effective brain delivery. Here we present the synthesis and in vitro stability of a series of N-methyl-N-benzylamide NSAID conjugates in various media, including human plasma and rat brain homogenate. Preliminary studies indicate that naproxen conjugates rapidly release the parent NSAID in plasma whereas indomethacin conjugates have plasma half-lives of several hours. These conjugates have the potential to improve the efficacy of CNS therapies by increasing the brain bioavailability of anti-inflammatory drugs.

In vitro stability of N-benzylamide non-steroidal anti-inflammatory drug conjugates

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.