Aspirin Derivatives Exploration: A Review on Comparison Study with Parent Drug

Abstract

In recent decades, drug modification is no longer unusual in the pharmaceutical world as living things are evolving in response to environmental changes. Aspirin as one of the non-steroidal anti-inflammatory drugs (NSAID) is a common over-the-counter drug due to its analgesic, antipyretic and anti-inflammatory activity. This review article highlights on the recent derivatives of aspirin, which were developed either to reduce the risk of side effects or to obtain better physicochemical properties. Aspirin derivatives can be synthesized in various pathways and have been reported to give better biological activities compared to the parent drug. Nitric oxide (NO)-aspirin gives a potent anticancer drug as it able to inhibit lung and prostate cancer cells. Meanwhile NOSH-aspirin that release hydrogen sulphide (H2S) and NO moiety is a potent anti-inflammatory agent that stimulate the gastric and colonic secretion, prevent the penetration of acid in gastrointestinal. It also has anticancer action that is effective in hindering the proliferation of pancreatic and colon cancer cells. Aspirin-thiourea has been studied its antimicrobial activity. Still, it resulted in poor inhibition due to steric hindrance of the compounds and influence its penetration into the enzyme’s active site. However, aspirin-amide has managed to inhibit the bacterial and fungal, and compound with halogen substituents is reported with the highest inhibition. Aspirin derivative linked with chalcone has poor antibacterial and antioxidant due bulky structure of the compounds, but it has a superior anticancer that induce cancer cells apoptosis by reactive oxygen species (ROS) treatment. The modification of azo-aspirin has more potential in antibacterial activity compared to ampicillin especially when the presence of halogens substituents is involved. Overall, these aspirin derivatives are safe to be considered as potential pharmaceutical agents.