2011/01/01 by Edon Vitaku, David T. Smith, Jón T. Njardarson +1 · 4 citations
Biochemistry, Genetics and Molecular Biology · Chemistry · Medicine · Nursing · #Consumer Attitudes and Food Labeling #Obesity, Physical Activity, Diet #Phenothiazines and Benzothiazines Synthesis and Activities #Sodium Intake and Health #Synthesis and Biological Evaluation #Synthesis of β-Lactam Compounds
paper · doi:10.1021/jm501100b
openalex publication_date 2011/01/01 · openalex created_date 2025/10/10 · openalex updated_date 2026/08/01
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.