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Ibuprofen and Lipoic Acid Diamides as Potential Codrugs with Neuroprotective Activity by Piera Sozio; Eleonora D'Aurizio; Antonio Iannitelli; Amelia Cataldi; Susi Zara; Franco Cantalamessa; Cinzia Nasuti; Antonio Di Stefano is a Chemistry article available to read on EtoBox.
What is Ibuprofen and Lipoic Acid Diamides as Potential Codrugs with Neuroprotective Activity about?
## Abstract Current evidences support the hypothesis that non‐steroidal anti‐inflammatory drugs (NSAIDs) and antioxidant therapy might protect against the development of Alzheimer's disease (AD). In the present work, our attention was focused on ibuprofen (IBU) used in clinical trails to prevent Alzheimer's disease, and (__R__)‐α‐lipoic acid (LA) considered as a potential neuroprotective agent in AD therapy. In particular, we investigated a series of lipophilic molecular combinations obtained by joining (__R__)‐α‐lipoic acid and ibuprofen via an amide bond. These new entities might allow targeted delivery of the parent drugs to neurons, where cellular oxidative stress and inflammation seem related to Alzheimer's disease. Our study included the synthesis of conjugates **1–3** and the evaluation of their physicochemical and __in‐vitro__ antioxidant properties. The new compounds are extremely stable in aqueous buffer solutions (pH = 1.3 and 7.4), and in rat and human plasma they showed a slow bioconversion to ibuprofen and (__R__)‐α‐lipoic acid. Codrugs **1–3** displayed __in vitro__ free radical scavenging activity and were hydrolyzed more rapidly in brain tissue than in rat serum in
Who reads Ibuprofen and Lipoic Acid Diamides as Potential Codrugs with Neuroprotective Activity?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Piera Sozio; Eleonora D'Aurizio; Antonio Iannitelli; Amelia Cataldi; Susi Zara; Franco Cantalamessa; Cinzia Nasuti; Antonio Di Stefano
- Publisher
- Wiley
- Published
- 2010
- Language
- EN
- Field
- Chemistry (Physical Sciences)