Related Experiment Video
Updated: Jan 14, 2026

Optimization of the Ugi Reaction Using Parallel Synthesis and Automated Liquid Handling
Published on: November 11, 2008
Ugi and Groebke-Blackburn-Bienaymé Reactions in Medicinal Chemistry: An Outlook on New Bioactive Compounds
Gustavo Barbosa-Reis1, Julia Lavorenti1, Bruna Lorentz Alves1
1Department of Chemistry - Institute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of São Paulo (UNIFESP), Diadema Campus, 275 Artur Riedel St., Diadema 09972-270, Brazil.
Abstract:
The FDA has approved 174 new molecular entities over the last 5 years. In 2023, the anticancer and infectious disease areas represented an impressive percentage of drug approvals, 24% and 9%, respectively, following the decade's trends. This reflects the pharmaceutical industry's increasing demand for novel compounds, particularly in these fields. Isocyanide-based multicomponent reactions, such as Ugi and Groebke-Blackburn-Bienaymé reactions, stand out for their versatility in obtaining different bioactive scaffolds using simpler starting materials. A large array of complex scaffold molecules can be obtained by using a multicomponent synthesis step. For this reason, this mini-review summarizes some recent works that employed this approach to afford new anticancer, antiviral, antimicrobial, and antiparasitic compounds. In each case, how the modifications impact activity or cytotoxicity is discussed. Also, the possible gaps that should be evaluated in further work are highlighted to inspire the design of new compounds.
More Related Videos
10:49Identification of Small Molecule-binding Proteins in a Native Cellular Environment by Live-cell Photoaffinity Labeling
Published on: September 20, 2016
09:04A Direct, Early Stage Guanidinylation Protocol for the Synthesis of Complex Aminoguanidine-containing Natural Products
Published on: September 9, 2016
Related Concept Videos
Cycloaddition Reactions: Overview
Drug Metabolism: Phase II Reactions
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Overview
Cycloaddition Reactions: MO Requirements for Thermal Activation
Reactions of Aldehydes and Ketones: Baeyer–Villiger Oxidation
The carbonyl center is activated by...
Drug Metabolism: Phase I Reactions