In multi-target drug design (MTD) medicinal chemistry aims to integrate multiple pharmacophores into a single
drug molecule in order to make it active on several molecular biological mechanisms simultaneously. Given the fact that
most diseases are multifactorial in nature, MTD is being pursued with increasing intensity, which has resulted in improved
outcomes in disease models and several compounds have entered clinical trials. In a wide range of examples we illustrate
how various functionalities have been combined within single structures and how this has affected their (pre)clinical outcome.
This review describes the successful application of MTD for disorders such as neurodegenerative, cardiovascular,
diabetes, metabolic and inflammatory diseases, especially focusing on the field of atherosclerosis where multi-target
strategies are a promising alternative to the classical “one target-one drug” design approach.
Keywords: Alzheimer’s disease, atherosclerosis, cardiovascular diseases, inflammation, metabolic syndrome, multifactorial
diseases, multifunctional molecules.
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