2. Academic Validation
  3. 1,2,4-Triazolo[1,5-a]pyrimidines in drug design

1,2,4-Triazolo[1,5-a]pyrimidines in drug design

  • Eur J Med Chem. 2019 Mar 1:165:332-346. doi: 10.1016/j.ejmech.2019.01.027.
Killian Oukoloff 1,  Bobby Lucero 2,  Karol R Francisco 2,  Kurt R Brunden 3,  Carlo Ballatore 4
Affiliations

Affiliations

  • 1 Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA, 92093, USA.
  • 2 Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA, 92093, USA.
  • 3 Center for Neurodegenerative Disease Research, Perelman School of Medicine, University of Pennsylvania, 3600 Spruce Street, Philadelphia, PA, 19104-6323, USA.
  • 4 Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA, 92093, USA. Electronic address: cballatore@ucsd.edu.
PMID: 30703745 DOI: 10.1016/j.ejmech.2019.01.027
Abstract

The 1,2,4-triazolo[1,5-a]pyrimidine (TP) heterocycle, in spite of its relatively simple structure, has proved to be remarkably versatile as evidenced by its use in many different applications reported over the years in different areas of drug design. For example, as the ring system of TPs is isoelectronic with that of purines, this heterocycle has been proposed as a possible surrogate of the purine ring. However, depending on the choice of substituents, the TP ring has also been described as a potentially viable bio-isostere of the carboxylic acid functional group and of the N-acetyl fragment of ε-N-acetylated lysine. In addition, the metal-chelating properties of the TP ring have also been exploited to generate candidate treatments for Cancer and parasitic diseases. In the present review article, we discuss recent applications of the TP scaffold in medicinal chemistry, and provide an overview of its properties and methods of synthesis.

Keywords

1,2,4-triazolo[1,5-a]pyrimidine; Heterocyclic chemistry; Medicinal chemistry.

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