1,2,4-Triazolo[1,5-a]pyrimidines in drug design.
3
Center for Neurodegenerative Disease Research, Perelman School of Medicine
5
3600 Spruce Street Philadelphia PA 19104-6323 USA
|
Publication type: Journal Article
Publication date: 2019-03-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
30703745
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
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.
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Total citations:
100
Citations from 2025:
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Oukoloff K. et al. 1,2,4-Triazolo[1,5-a]pyrimidines in drug design. // European Journal of Medicinal Chemistry. 2019. Vol. 165. pp. 332-346.
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Oukoloff K., Lucero B., Francisco K. R., Brunden K. R., Ballatore C. 1,2,4-Triazolo[1,5-a]pyrimidines in drug design. // European Journal of Medicinal Chemistry. 2019. Vol. 165. pp. 332-346.
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TY - JOUR
DO - 10.1016/j.ejmech.2019.01.027
UR - https://doi.org/10.1016/j.ejmech.2019.01.027
TI - 1,2,4-Triazolo[1,5-a]pyrimidines in drug design.
T2 - European Journal of Medicinal Chemistry
AU - Oukoloff, Killian
AU - Lucero, Bobby
AU - Francisco, Karol R.
AU - Brunden, K. R.
AU - Ballatore, C.
PY - 2019
DA - 2019/03/01
PB - Elsevier
SP - 332-346
VL - 165
PMID - 30703745
SN - 0223-5234
SN - 1768-3254
ER -
Cite this
BibTex (up to 50 authors)
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@article{2019_Oukoloff,
author = {Killian Oukoloff and Bobby Lucero and Karol R. Francisco and K. R. Brunden and C. Ballatore},
title = {1,2,4-Triazolo[1,5-a]pyrimidines in drug design.},
journal = {European Journal of Medicinal Chemistry},
year = {2019},
volume = {165},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.ejmech.2019.01.027},
pages = {332--346},
doi = {10.1016/j.ejmech.2019.01.027}
}