Bioactive Compounds through Structural Modification of Natural Products

Dear Colleagues,

Pharmacological activity and druggability are two essential factors for drug innovation. The pharmacological activity is indispensable, and the druggability is determined by the physico-chemical, biochemical, pharmacokinetic and safety properties of drugs. Natural products are a rich source of therapeutic drugs. They are unusually featured by structural diversity. The structural modification of natural products should result in a synthesis process ready for industrialization, protect the environment and resources, realize chemical modifications according to the molecular size and complexity of natural products, acquire novel structures through structure–activity relationship analysis, pharmacophore definition, and scaffold hopping. The strategy for structural modification is to increase potency and selectivity, improve physico-chemical, biochemical and pharmacokinetic properties, eliminate or reduce side effects, and attain intellectual properties. This Special Issue will focus on papers showing data with new molecules obtained after molecular modifications in natural products, on the synthesis and/or biological effects of new compounds designed using medicinal chemistry approaches looking to improve the activities of original molecules obtained from natural products against worldwide diseases, including, but not limited to, neglected diseases, chronic inflammatory diseases, cancer, tropical diseases (malaria, leishmaniosis, dengue, zika), neurological diseases, cancer, and COVID-19.

Dr. Patricia Dias Fernandes
Guest Editor

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