Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals : Miniperspective
There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.
Abstract
Nitrogen heterocycles are among the most significant structural components of pharmaceuticals.
Analysis of our database of U.S. FDA approved drugs reveals that 59% of unique small-molecule
drugs contain a nitrogen heterocycle. In this review we report on the top 25 most
commonly utilized nitrogen heterocycles found in pharmaceuticals. The main part of
our analysis is divided into seven sections: (1) three- and four-membered heterocycles,
(2) five-, (3) six-, and (4) seven- and eight-membered heterocycles, as well as (5)
fused, (6) bridged bicyclic, and (7) macrocyclic nitrogen heterocycles. Each section
reveals the top nitrogen heterocyclic structures and their relative impact for that
ring type. For the most commonly used nitrogen heterocycles, we report detailed substitution
patterns, highlight common architectural cores, and discuss unusual or rare structures.