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Amide bonds represent crucial functional groups in numerous biomolecules and pharmaceuticals, characterized by distinct structures and properties, and are essential for drug synthesis. By employing a bioisosteric replacement strategy, innovative drug architectures can be devised that circumvent existing patent protections, thereby offering an effective avenue for the discovery of new drug candidates. This review primarily introduces the current synthetic methodologies for amides and their bioisosteres. Additionally, it discusses the advantages and disadvantages associated with various functional groups. A comparative analysis of the differing properties of amides and their bioisosteres within compounds is also presented.
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