Health & Environmental Research Online (HERO)


Print Feedback Export to File
7064117 
Journal Article 
1,2,4-Triazolo[1,5-a]pyrimidines in drug design 
Oukoloff, K; Lucero, B; Francisco, KR; Brunden, KR; Ballatore, C; , 
2019 
Yes 
European Journal of Medicinal Chemistry
ISSN: 0223-5234
EISSN: 1768-3254 
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER 
ISSY-LES-MOULINEAUX 
332-346 
30703745 
WOS:000459358600024 
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 bioisostere of the carboxylic acid functional group and of the N-acetyl fragment of epsilon-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. (C) 2019 Elsevier Masson SAS. All rights reserved.