Trimetazidine is the first registered drug belonging to the class of antianginal agents specifically classified as a metabolic modulator. It protects the heart from ischemic damage and oxidative stress. Clinically, it has demonstrated significant benefits for patients with coronary artery disease, showing a prophylactic effect against angina attacks. Its lack of hemodynamic action makes it suitable for combination therapy with other antianginal drugs. Beyond its cardioprotective effects, trimetazidine has also shown therapeutic potential in various renal disorders and the treatment of atherosclerosis. Derivatives of 2-arylpropionic acid represent one of the most widely used classes of nonsteroidal anti-inflammatory drugs (NSAIDs), valued for their anti-inflammatory, analgesic, and antipyretic properties. These compounds exhibit metabolic chiral inversion, and the enantiomers often show distinct pharmacological activities. Compounds containing amide functional groups are of particular interest to both pharmaceutical research and human health due to their fundamental role in the design of new therapeutic agents. This work presents the synthesis and characterization of novel hybrid molecules combining trimetazidine with various profens (ibuprofen, ketoprofen, naproxen, etc.). The target compounds are designed to offer dual pharmacological action—addressing both ischemic cardiovascular conditions and inflammatory diseases. These newly synthesized derivatives show promising potential for future pharmaceutical development and therapeutic application.