Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles
Natalya Agafonova
1
,
Yanina Burgart
1
,
Victor Saloutin
1
,
Alexandra Trefilova
2
,
Sergey Solodnikov
2
,
Vera Maslova
2
,
Olga Krasnykh
2
,
Sophia Borisevich
3
,
Sergey Khursan
3
2
Publication type: Journal Article
Publication date: 2019-07-02
scimago Q3
wos Q3
SJR: 0.380
CiteScore: 4.5
Impact factor: 2.6
ISSN: 15734064, 18756638, 21610444, 00766054
PubMed ID:
30398121
Drug Discovery
Abstract
Background:
Formally belonging to the non-steroidal anti-inflammatory drug class pyrazolones have long been used in medical practices.
Objective:
Our goal is to synthesize N-methylated 1-aryl-3-polyfluoroalkylpyrazolones as fluorinated analogs of antipyrine, their isomeric O-methylated derivatives resembling celecoxib structure and evaluate biological activities of obtained compounds.
Methods:
In vitro (permeability) and in vivo (anti-inflammatory and analgesic activities, acute toxicity, hyperalgesia, antipyretic activity, “open field” test) experiments. To suggest the mechanism of biological activity, molecular docking of the synthesized compounds was carried out into the tyrosine site of COX-1/2.
Conclusion:
The trifluoromethyl antipyrine represents a valuable starting point in design of the lead series for discovery new antipyretic analgesics with anti-inflammatory properties.
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Agafonova N. et al. Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles // Medicinal Chemistry. 2019. Vol. 15. No. 5. pp. 521-536.
GOST all authors (up to 50)
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Agafonova N., Shchegolkov E., Burgart Y., Saloutin V., Trefilova A., Triandafilova G., Solodnikov S., Maslova V., Krasnykh O., Borisevich S., Khursan S. Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles // Medicinal Chemistry. 2019. Vol. 15. No. 5. pp. 521-536.
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RIS
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TY - JOUR
DO - 10.2174/1573406414666181106145435
UR - https://doi.org/10.2174/1573406414666181106145435
TI - Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles
T2 - Medicinal Chemistry
AU - Agafonova, Natalya
AU - Shchegolkov, Evgeny
AU - Burgart, Yanina
AU - Saloutin, Victor
AU - Trefilova, Alexandra
AU - Triandafilova, Galina
AU - Solodnikov, Sergey
AU - Maslova, Vera
AU - Krasnykh, Olga
AU - Borisevich, Sophia
AU - Khursan, Sergey
PY - 2019
DA - 2019/07/02
PB - Bentham Science Publishers Ltd.
SP - 521-536
IS - 5
VL - 15
PMID - 30398121
SN - 1573-4064
SN - 1875-6638
SN - 2161-0444
SN - 0076-6054
ER -
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BibTex (up to 50 authors)
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@article{2019_Agafonova,
author = {Natalya Agafonova and Evgeny Shchegolkov and Yanina Burgart and Victor Saloutin and Alexandra Trefilova and Galina Triandafilova and Sergey Solodnikov and Vera Maslova and Olga Krasnykh and Sophia Borisevich and Sergey Khursan},
title = {Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles},
journal = {Medicinal Chemistry},
year = {2019},
volume = {15},
publisher = {Bentham Science Publishers Ltd.},
month = {jul},
url = {https://doi.org/10.2174/1573406414666181106145435},
number = {5},
pages = {521--536},
doi = {10.2174/1573406414666181106145435}
}
Cite this
MLA
Copy
Agafonova, Natalya, et al. “Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles.” Medicinal Chemistry, vol. 15, no. 5, Jul. 2019, pp. 521-536. https://doi.org/10.2174/1573406414666181106145435.