Open Access
Microwave-Assisted Synthesis of 3-Hydroxy-2-oxindoles and Pilot Evaluation of Their Antiglaucomic Activity
Alexander M. Efremov
1, 2
,
Olga Beznos
3
,
Roman O. Eremeev
1
,
Natalia B Chesnokova
3
,
Elena R. Milaeva
1, 2
,
E. F. Shevtsova
2
,
Natalia A Lozinskaya
1
3
Helmholtz National Medical Center of Eye Diseases, 14/19 Sadovaya-Chernogryazskaya St., Moscow 105062, Russia
|
Publication type: Journal Article
Publication date: 2023-03-07
scimago Q1
wos Q1
SJR: 1.273
CiteScore: 9.0
Impact factor: 4.9
ISSN: 16616596, 14220067
PubMed ID:
36982181
Catalysis
Organic Chemistry
Inorganic Chemistry
Physical and Theoretical Chemistry
Computer Science Applications
Spectroscopy
Molecular Biology
General Medicine
Abstract
Glaucoma is a widespread neurodegenerative disease for which increased intraocular pressure (IOP) is a primary modifiable risk factor. Recently, we have observed that compounds with oxindole scaffolds are involved in the regulation of intraocular pressure and therefore have potential antiglaucomic activity. In this article, we present an efficient method for obtaining novel 2-oxindole derivatives via microwave-assisted (MW) decarboxylative condensation of substituted isatins with malonic and cyanoacetic acids. Various 3-hydroxy-2-oxindoles were synthesized using MW activation for 5–10 min with high yields (up to 98%). The influence of novel compounds applied in instillations on IOP was studied in vivo on normotensive rabbits. The lead compound was found to reduce the IOP by 5.6 Torr (ΔIOP for the widely used antiglaucomatousic drug timolol 3.5 Torr and for melatonin 2.7 Torr).
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10
Total citations:
10
Citations from 2025:
3
(30%)
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GOST
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Efremov A. M. et al. Microwave-Assisted Synthesis of 3-Hydroxy-2-oxindoles and Pilot Evaluation of Their Antiglaucomic Activity // International Journal of Molecular Sciences. 2023. Vol. 24. No. 6. p. 5101.
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Efremov A. M., Beznos O., Eremeev R. O., Chesnokova N. B., Milaeva E. R., Shevtsova E. F., Lozinskaya N. A. Microwave-Assisted Synthesis of 3-Hydroxy-2-oxindoles and Pilot Evaluation of Their Antiglaucomic Activity // International Journal of Molecular Sciences. 2023. Vol. 24. No. 6. p. 5101.
Cite this
RIS
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TY - JOUR
DO - 10.3390/ijms24065101
UR - https://doi.org/10.3390/ijms24065101
TI - Microwave-Assisted Synthesis of 3-Hydroxy-2-oxindoles and Pilot Evaluation of Their Antiglaucomic Activity
T2 - International Journal of Molecular Sciences
AU - Efremov, Alexander M.
AU - Beznos, Olga
AU - Eremeev, Roman O.
AU - Chesnokova, Natalia B
AU - Milaeva, Elena R.
AU - Shevtsova, E. F.
AU - Lozinskaya, Natalia A
PY - 2023
DA - 2023/03/07
PB - MDPI
SP - 5101
IS - 6
VL - 24
PMID - 36982181
SN - 1661-6596
SN - 1422-0067
ER -
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BibTex (up to 50 authors)
Copy
@article{2023_Efremov,
author = {Alexander M. Efremov and Olga Beznos and Roman O. Eremeev and Natalia B Chesnokova and Elena R. Milaeva and E. F. Shevtsova and Natalia A Lozinskaya},
title = {Microwave-Assisted Synthesis of 3-Hydroxy-2-oxindoles and Pilot Evaluation of Their Antiglaucomic Activity},
journal = {International Journal of Molecular Sciences},
year = {2023},
volume = {24},
publisher = {MDPI},
month = {mar},
url = {https://doi.org/10.3390/ijms24065101},
number = {6},
pages = {5101},
doi = {10.3390/ijms24065101}
}
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MLA
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Efremov, Alexander M., et al. “Microwave-Assisted Synthesis of 3-Hydroxy-2-oxindoles and Pilot Evaluation of Their Antiglaucomic Activity.” International Journal of Molecular Sciences, vol. 24, no. 6, Mar. 2023, p. 5101. https://doi.org/10.3390/ijms24065101.
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