Related Experiment Video
Updated: Nov 12, 2025

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Recent Developments on the Synthesis and Biological Activities of Fused Pyrimidinone Derivatives
Pule Seboletswe1, Paul Awolade1, Parvesh Singh1
1School of Chemistry and Physics, University of Kwa-Zulu Natal, Private Bag X01, Scottsville, Durban, South Africa.
Abstract:
Heterocyclic compounds constitute a unique class of organic compounds endowed with a wide range of synthetic and pharmaceutical applications. Pyrimidinones and their fused analogues have received focused attention in this regard, partly due to their mimicry of nucleobases which consequently forges their interesting medicinal properties. Over the years, the medicinal chemistry research community has experienced an upsurge in articles describing the exploration of these scaffolds to develop effective therapeutic agents. Several biological activities, including antimicrobial, antiviral, anticancer, antidiabetic, anti-inflammatory, anticonvulsive, and antihistaminic, have been well documented. This minireview presents a compendium of recent developments (2017-2020) focused on the synthesis and biological activities of fused pyrimidinones. The goal is to update medicinal chemists on the therapeutic relevance of fused pyrimidinones and the molecular architecture of clinic-worthy drug candidates. A brief account of the structure-activity relationships (SAR) revealed from different biological assays is also discussed.
Related Concept Videos
Biosynthesis of Nucleic Acids
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Five-Membered Heterocyclic Aromatic Compounds: Overview
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Overview
Basicity of Heterocyclic Aromatic Amines
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...

