Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry

Overview

Journal J Med Chem

Publisher American Chemical Society

Specialty Chemistry

Date 2019 Dec 3

PMID 31789518

Citations 53

Authors

Arun K Ghosh

Margherita Brindisi

Affiliations

Soon will be listed here.

Abstract

The urea functionality is inherent to numerous bioactive compounds, including a variety of clinically approved therapies. Urea containing compounds are increasingly used in medicinal chemistry and drug design in order to establish key drug-target interactions and fine-tune crucial drug-like properties. In this perspective, we highlight physicochemical and conformational properties of urea derivatives. We provide outlines of traditional reagents and chemical procedures for the preparation of ureas. Also, we discuss newly developed methodologies mainly aimed at overcoming safety issues associated with traditional synthesis. Finally, we provide a broad overview of urea-based medicinally relevant compounds, ranging from approved drugs to recent medicinal chemistry developments.

Citing Articles

Molecular Recognition of Diaryl Ureas in Their Targeted Proteins-A Data Mining and Quantum Chemical Study.

Aljohani M, Hu X Molecules. 2025; 30(5).

PMID: 40076232 PMC: 11902014. DOI: 10.3390/molecules30051007.

Discovery of Novel Pyridin-2-yl Urea Inhibitors Targeting ASK1 Kinase and Its Binding Mode by Absolute Protein-Ligand Binding Free Energy Calculations.

Wang L, Gao Y, Chen Y, Tang Z, Lin X, Bai M Int J Mol Sci. 2025; 26(4).

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Synthesis, Characterization, and Antimicrobial Activity of Urea-Containing α/β Hybrid Peptides against and Methicillin-Resistant .

Firdous S, Sarkar A, Manhas R, Chowdhary R, Rathore A, Kumari J ACS Omega. 2025; 10(2):2102-2115.

PMID: 39866621 PMC: 11755142. DOI: 10.1021/acsomega.4c08680.

Non-phosgene route: catalytic carbonylation of amines to form unsymmetrical ureas.

Xie S, Wang Y Natl Sci Rev. 2025; 12(1):nwae450.

PMID: 39781275 PMC: 11708213. DOI: 10.1093/nsr/nwae450.

Design, Synthesis, and Biological Evaluation of Novel Urea-Containing Carnosic Acid Derivatives with Anticancer Activity.

Moura S, Marin S, Rufino I, Guedes R, Cascante M, Salvador J Int J Mol Sci. 2025; 25(24.

PMID: 39769100 PMC: 11728001. DOI: 10.3390/ijms252413332.

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