Medicinal chemistry strategies to extend duration of action of inhaled drugs for intracellular targets

Bioorg Med Chem Lett. 2022 Apr 15:62:128627. doi: 10.1016/j.bmcl.2022.128627. Epub 2022 Feb 12.


Prolonging duration of action of inhaled drugs is a challenging endeavor and guidance for medicinal chemistry teams is very limited, particularly if the site of action is intracellular. Herein, we identified recent literature reports of newly designed inhaled compounds with intracellular targets and summarized learnings from different approaches and strategies undertaken by medicinal chemistry teams. We highlight key properties that have shown to lead to longer duration of action and provide guidance on the best strategy to follow while designing a new inhaled drug with an intracellular target.

Keywords: Drug design; Duration of action; Inhaled drugs; Intracellular targets; Pharmacokinetics; Pulmonary.

Publication types

  • Review

MeSH terms

  • Chemistry, Pharmaceutical*