Journal of Medicinal Chemistry· 2014Q1· Review
Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals
- 6,286citations
- Q1SCImago
- 2014year
Short summary
Nitrogen heterocycles are crucial in drug design, with 59% of U.S. FDA-approved small-molecule drugs containing them.
AI-generated from the title and abstract; the full text is not read.
Key points
- 59% of U.S. FDA-approved small-molecule drugs contain nitrogen heterocycles.
- The review categorizes and analyzes the top 25 most common nitrogen heterocycles.
- Detailed substitution patterns and common architectural cores are highlighted.
- Analysis covers diverse ring systems from small to macrocyclic and fused structures.
AI-generated from the title and abstract; the full text is not read.
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.
The authors' abstract, as published at the source. Journal of Medicinal Chemistry, 2014 · DOI ↗
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Field: Organic Chemistry
Organic ChemistryChemistry