Strategic Use of the Necessary Nitrogen Atom for Holistic Property-Based Drug Design.

Authors

Lewis D Pennington, Julia M Clay, Sandrine M Hell, Matthew J Hesse, Elizabeth V Jones, Rory C McAtee, Theodore D Michels, Alshaima'a M Qunies

Published in

Journal of medicinal chemistry. Volume 69. Issue 16. Pages 19547-19559. Aug 27, 2026.

Abstract

Property-based drug design has advanced considerably since its emergence following the publication of the rule-of-5 in 1997. We show in this perspective that the classical bioisosteric exchange of an aromatic methine group with a nitrogen atom has broad utility in the modern context of drug multiparameter optimization. We also demonstrate how the "necessary nitrogen atom" can be leveraged for holistic property-based drug design, and include a historical overview, key concepts, and real-world case studies.

PMID:
42679143
Bibliographic data and abstract were imported from PubMed on 02 Sep 2026.

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