The Substitute Groups in FDA-Approved Small Molecule Drugs in 2020 - 2024.

The strategic application of substituents is a cornerstone of modern drug discovery, critical for fine-tuning efficacy, safety, and pharmacokinetics. This review systematically catalogs the landscape of functional groups in FDA-approved small molecules (2020-2024), deciphering the rationale behind their use. Through case studies, it translates observed trends into practical design principles for medicinal chemists, highlighting how specific substituents address key challenges in developing novel therapeutics.