<![CDATA[Molecular modification of natural compounds is an important pillar in modern drug discovery because it is able to overcome the intrinsic limitations of natural compounds, such as low solubility, poor bioavailability, or high toxicity. This literature review aims to summarize various structural modification strategies, including functional group derivatization, fragmentation, and simplification, as well as examine their impact on the Structure-Activity Relationship (SAR). The research method was conducted through a comprehensive literature search on relevant scientific databases. The results of the study show that appropriate chemical modifications can significantly increase therapeutic potential, optimize pharmacokinetic profiles (ADME), and minimize side effects. In addition, the integration of the filtration of natural material compounds with synthetic chemical approaches has proven to be an effective strategy in the development of new and more potent chemical entities. These findings confirm that molecular modification not only plays a role in correcting the weaknesses of natural compounds, but also opens up innovation opportunities in the design of medicines based on natural ingredients. Thus, this research makes a conceptual contribution to the development of sustainable and scientifically based modern medicine. ]]>
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