AI Article Synopsis
- Pharmacotherapy is crucial for treating and preventing cerebral ischemia, but current drugs face challenges like poor absorption, low solubility, and rapid metabolism that limit their efficacy.
- To address these issues, researchers are using prodrug strategies that convert inactive drug forms into active ones, enhancing brain permeability and reducing toxicity.
- This review highlights effective prodrug developments over the last two decades, aiming to improve treatment outcomes for cerebral ischemia and providing insights for pharmaceutical chemists.
Article Abstract
It is well-known that pharmacotherapy plays a pivotal role in the treatment and prevention of cerebral ischemia. Nevertheless, existing drugs, including numerous natural products, encounter various challenges when applied in cerebral ischemia treatment. These challenges comprise poor brain absorption due to low blood-brain barrier (BBB) permeability, limited water solubility, inadequate bioavailability, poor stability, and rapid metabolism. To address these issues, researchers have turned to prodrug strategies, aiming to mitigate or eliminate the adverse properties of parent drug molecules. In vivo metabolism or enzymatic reactions convert prodrugs into active parent drugs, thereby augmenting BBB permeability, improving bioavailability and stability, and reducing toxicity to normal tissues, ultimately aiming to enhance treatment efficacy and safety. This comprehensive review delves into multiple effective prodrug strategies, providing a detailed description of representative prodrugs developed over the past two decades. It underscores the potential of prodrug approaches to improve the therapeutic outcomes of currently available drugs for cerebral ischemia. The publication of this review serves to enrich current research progress on prodrug strategies for the treatment and prevention of cerebral ischemia. Furthermore, it seeks to offer valuable insights for pharmaceutical chemists in this field, offer guidance for the development of drugs for cerebral ischemia, and provide patients with safer and more effective drug treatment options.
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| http://dx.doi.org/10.1016/j.ejmech.2024.116457 | DOI Listing |
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