Title:N-Heterocycles as Privileged Scaffolds in FDA Approved Different NMEs
of 2021: A Review
Volume: 20
Issue: 4
Author(s): Faryal Chaudhry*, Rubina Munir and Nayab Malik
Affiliation:
- Department of Chemistry, Kinnaird College for Women, 93 Jail Road, Lahore 54000, Pakistan
Keywords:
ADME, Aza-heterocycles, disease, drug discovery, FDA, new molecular entities, heterocyclic compounds.
Abstract: The presence of N-heterocyclic ring systems as promising features in the molecular skeleton
of FDA-approved drugs, underlie the remarkable contributions of these heterocyclic nuclei in the
field of medicine. Despite instability risks associated with the COVID pandemic, the US FDA approved
50 drugs (36 NMEs and 14 biological products) in the year 2021. The active ingredients of 32
drugs out of these 36 NMEs (almost 89%) contain saturated, partially unsaturated and aromatic Nheterocyclic
moieties in their molecular assemblies, hence dominating the medicinal approvals. While
27 molecules (75% of these NMEs drugs) are prominent small NMEs. Herein, we have considered
profiling those FDA-approved 27 small-molecule drugs which are decorated with N-heterocycles as
privileged scaffolds. These drugs are grouped on the basis of a number of N-heterocycles present in
their structural framework. The spectrum of these drugs in terms of their structural features and medicinal
importance is summarized in this review. Also, the pertinent analyses of their drug-likeliness
conferring some general pharmacokinetic principles are highlighted.
