Related Experiment Video
Updated: Jan 28, 2026

Synthesis of Protein Bioconjugates via Cysteine-maleimide Chemistry
Published on: July 20, 2016
Imidazo[1,2‑a]pyridines in Medicinal Chemistry: Recent Advances in Synthesis and Biological Activities
Larissa A P Ferreira1, Lucas Caruso1, Nathalia F Nadur1
1Laboratory of Molecular Diversity and Medicinal Chemistry (LaDMol-QM), Department of Organic Chemistry, Institute of Chemistry, Federal Rural University of Rio de Janeiro, BR465, Km7, Seropédica,Rio de Janeiro 23897-000, Brazil.
Abstract:
Imidazo-[1,2-a]-pyridines are widely recognized scaffolds present in several marketed drugs, including the anxiolytics alpidem, saripidem, necopidem, and zolpidem, which are some of the most prescribed medications for insomnia. In this review, we analyze publication trends, which reveal exponential growth in research involving this scaffold. We highlight recent synthetic strategies (2017-2025) for the preparation of imidazo-[1,2-a]-pyridine derivatives, such as condensation, multicomponent and tandem reactions, intramolecular cyclizations, and oxidative couplings under green conditions. In addition, we discuss innovative Medicinal Chemistry studies exploring their applications in the treatment of cancer, Alzheimer's disease, tuberculosis, and neglected tropical diseases. Significant advances have been made in identifying derivatives with potent activity against specific biological targets, including kinases, tubulin, HDACs, the cytochrome bc1 complex of Mycobacterium tuberculosis, and key enzymes involved in the pathogenesis of Alzheimer's disease, such as cholinesterases and secretases. Altogether, this review consolidates the vast therapeutic potential of the imidazo-[1,2-a]-pyridine core, emphasizing its synthetic versatility and broad spectrum of biological activities, which firmly establish it as a privileged scaffold for drug discovery.
Related Concept Videos
Local Anesthetics: Chemistry and Structure-Activity Relationship
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
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...
What is Conservation Biology?
Chemistry of the Cell
Water
The polarity of the water molecule and its resulting hydrogen bonding makes water a unique substance with special properties that are intimately tied to the processes of life. Life originally evolved in an aqueous environment, and most of an organism’s cellular chemistry and metabolism occur inside the aqueous contents of the cell’s cytoplasm. Special properties of water are its high heat capacity...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...

