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.

Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals

The therapeutic journey of benzimidazoles: a review.

Microbially Produced Imidazole Propionate Impairs Insulin Signaling through mTORC1.

Mucoadhesive polymers in the design of nano-drug delivery systems for administration by non-parenteral routes: A review

Benzimidazole: an emerging scaffold for analgesic and anti-inflammatory agents.

Imidazole and benzimidazole rings are the most important nitrogen-containing heterocycles, which are widely explored and utilized by the pharmaceutical industry for drug discovery. Due to their special structural features and electron-rich environment, imidazole- and benzimidazole-containing drugs bind to a variety of therapeutic targets, thereby exhibiting a broad spectrum of bioactivities. Numerous imidazole- and benzimidazole-based drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potential. Due to their enormous medicinal value, the research and development of imidazole- and benzimidazole-containing drugs is an increasingly active and attractive topic of medicinal chemistry. This review enlightens the landscape of the discovery and development of imidazole- and benzimidazole-based drugs with an emphasis on structure activity relationship features (SAR), medicinal chemistry, and their mechanism of action. Furthermore, the present review also provides the recent advances in the development of imidazole- and benzimidazole-based drugs along with new perspectives. We hope that this paper will open up new opportunities for researchers to design future generation novel and potent imidazole- and benzimidazole-containing drugs.

Development of drugs based on imidazole and benzimidazole bioactive heterocycles: recent advances and future directions

Synthesis and pharmacological evaluation of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives as anti-inflammatory and analgesic agents

Monika Gaba

Papers

Benzimidazole: an emerging scaffold for analgesic and anti-inflammatory agents.

Development of drugs based on imidazole and benzimidazole bioactive heterocycles: recent advances and future directions

Synthesis and pharmacological evaluation of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives as anti-inflammatory and analgesic agents

Benzimidazole derivatives: search for GI-friendly anti-inflammatory analgesic agents

Synthesis, antimicrobial and cytotoxic activity of novel azetidine-2-one derivatives of 1H-benzimidazole